Insecticidal, acaricidal and fungicidal aminopyrimidines

ABSTRACT

Compounds of the formula: ##STR1## wherein A, Q and R 2  to R 5  are as defined in the text, compositions containing them and methods for using them to control insects, acarids and fungi.

CROSS-REFERENCE TO RELATED APPLICATIONS

This application is a 371 of PCT/US91/08241, filed Nov. 13, 1991, whichis a continuation-in-part of application Ser. No. 07/615,509, filed onNov. 19, 1990, now abandoned.

BACKGROUND OF THE INVENTION

1. Field of the Invention

This invention concerns aralkylamino-pyrimidines, pesticidalcompositions containing said compounds and use of the compounds tocontrol pests.

2. State of the Art

U.S. Pat. No. 4,895,849 discloses aralkylaminopyrimidine derivatives ofFormula I as insecticides, acaricides and fungicides ##STR2## wherein: Ais an alkylene group optionally substituted with one or two substituentsselected from the group alkynyl, haloalkyl, alkoxy, alkylthio and C₃ -C₅cycloalkyl.

EPA 370,704 discloses aralkylaminopyrimidine derivatives of the formula##STR3## wherein: R₅ is H, lower alkyl, cycloalkyl or lower haloalkyl.

EP 323,757 discloses alkylaminopyrimidine derivatives, process forproducing the same, and insecticide, acaricide and fungicides containingthe same as an active ingredient.

U.S. Pat. No. 4,435,402 discloses aminopyrimidine derivatives, processesfor their preparation, and fungicidal, insecticidal and acaricidalcompositions containing them.

EP 196,524 discloses phenoxyalkylamino-pyrimidine derivatives.

SUMMARY OF THE INVENTION

The invention pertains to compounds of Formula I, including allgeometric and stereoisomers, agriculturally suitable salts thereof,agricultural compositions containing them and their use as insecticides,acaricides and fungicides in both agronomic and nonagronomicenvironments. The compounds of the invention are: ##STR4## wherein: Q isselected from the group ##STR5## A is selected from the group C₁ -C₅alkylene and C₃ -C₆ cycloalkylene, where any one atom of A can beoptionally substituted with R¹ ;

G is O or S;

X is Si or Ge;

R¹ is selected from the group C₁ -C₂ haloalkyl, CN, C(O)R⁸, CO₂ R⁸,C(O)N(R⁸)R⁹, N₃, NO₂, N(R⁸)R⁹, N(R⁸)C(O)R⁹, N(R⁸)C(O)N(R¹⁰)R⁹,N(R⁸)S(O)₂ R¹⁰, OR⁸. OC(O)R⁸, OCO₂ R⁸, OC(O)N(R⁸)R⁹, OS(O)₂ R⁸, SR⁸,S(O)R⁸, S(O)₂ R⁸ and SCN; provided that when R¹ is N(R⁸)S(O)₂ R¹⁰, thenR¹⁰ is other than H and when R¹ is OC(O)R⁸, OCO₂ R⁸, OS(O)₂ R⁸, S(O)R⁸or S(O)₂ R⁸, then R⁸ is other than H;

R² is selected from the group H, halogen, C₁ -C₄ alkyl and C₁ -C₄haloalkyl;

R³ is selected from the group H, halogen, C₁ -C₆ alkyl, C₁ -C₆haloalkyl, C₂ -C₆ alkoxyalkyl and C₂ -C₆ alkylthioalkyl;

R⁴ is selected from the group halogen, C₁ -C₆ alkyl, C₁ -C₆ haloalkyl,C₂ -C₆ alkoxyalkyl and C₂ -C₆ alkylthioalkyl;

R⁵ is selected from the group H, HCO, C₂ -C₆ alkoxyalkyl C₂ -C₆alkylcarbonyl, C₂ -C₆ alkoxycarbonyl, C₂ -C₆ haloalkoxycarbonyl,C(O)R¹⁵, R¹¹ OC(O)N(R¹²)S--, R¹¹ (R¹²)NS--, and SR⁸ ; or R⁵ is C₁ -C₆alkyl optionally substituted with a group selected from halogen, CN,NO₂, S(O)_(n) R¹¹, C(O)R¹¹, CO₂ R¹¹, C₁ -C₃ haloalkoxy and phenyloptionally substituted by halogen, CN, or C₁ -C₂ haloalkyl;

R⁶ is selected from the group H, C₁ -C₆ alkyl, C₁ -C₆ alkoxy, C₂ -C₆alkoxyalkyl, C₂ -C₆ alkoxyalkoxy, C₂ -C₆ alkenyl, C₂ -C₆ haloalkenyl, C₂-C₆ alkynyl, C₂ -C₆ alkenyloxy, C₂ -C₆ alkynyloxy, C₃ -C₆ cycloalkyl, C₃-C₆ cycloalkylalkyl, C₁ -C₆ alkylthio, C₁ -C₆ alkylsulfinyl, C₁ -C₆alkylsulfonyl, C₁ -C₆ haloalkylthio, C₁ -C₆ haloalkylsulfinyl, C₁ -C₆haloalkylsulfonyl, phenyl optionally substituted with W and phenoxyoptionally substituted with W;

R⁷ is selected from the group H, halogen, CN, NO₂, C₁ -C₂ alkyl, C₁ -C₂alkoxy and CF₃ ;

R⁸ and R¹⁰ are independently selected from the group H, C₁ -C₆ alkyl, C₁-C₆ haloalkyl, C₂ -C₆ alkenyl, C₂ -C₆ haloalkenyl, C₂ -C₆ alkynyl, C₃-C₆ haloalkynyl, C₂ -C₆ alkoxyalkyl, C₂ -C₆ alkylthioalkyl, C₁ -C₆nitroalkyl, C₂ -C₆ cyanoalkyl, C₃ -C₈ alkoxycarbonylalkyl, C₃ -C₆cycloalkyl, C₃ -C₆ halocycloalkyl, phenyl optionally substituted with 1to 3 substituents independently selected from W and benzyl optionallysubstituted with 1 to 3 substituents independently selected from W;

R⁹ is selected from the group H and C₁ -C₄ alkyl;

R⁸ and R⁹ can be taken together when attached to the same atom as--(CH₂)₄ --, --(CH₂)₅ -- or --CH₂ CH₂ OCH₂ CH₂ --;

R¹¹ and R¹² are independently selected from the group C₁ -C₄ alkyl;

R¹³ is selected from the group C₁ -C₄ alkyl, C₁ -C₄ alkoxyalkyl andphenyl optionally substituted with W;

R¹⁴ is selected from the group C₁ -C₆ alkyl, C₁ -C₆ alkoxy, C₁ -C₆haloalkoxy, and phenyl or benzyl, each phenyl and benzyl optionally andindependently substituted with 1 to 3 W;

R¹⁵ is selected from the group ##STR6## W is selected from the grouphalogen, CN, NO₂, C₁ -C₂ alkyl, C₁ -C₂ haloalkyl, C₁ -C₂ alkoxy, C₁ -C₂haloalkoxy, C₁ -C₂ alkylthio, C₁ -C₂ haloalkylthio, C₁ -C₂ alkylsulfonyland C₁ -C₂ haloalkylsulfonyl; and

n is 0, 1 or 2;

provided that:

i) when Q is Q-1 and A is C₁ -C₅ alkylene, then A is substituted with R¹;

ii) when Q is Q-1, A is C₁ -C₅ alkylene and R¹ is OR⁸ or SR⁸, then R⁸ isother than C₁ -C₆ alkyl; and

iii) when Q is Q-1 and A is C₁ -C₅ alkylene, then R¹ is other than C₁-C₂ haloalkyl.

Preferred Compounds A are those compounds of Formula I wherein:

A is C₁ -C₅ alkylene;

G is S;

R¹ is selected from the group OR⁸, OC(O)R⁸ and SR⁸ ;

R² is H;

R³ is C₁ -C₆ alkyl;

R⁴ is halogen;

R⁵ is selected from the group H and CH₃ ;

R⁶ is selected from the group C₁ -C₆ alkyl, C₂ -C₆ alkoxyalkyl, C₂ -C₆alkoxyalkoxy and phenoxy optionally substituted with W;

R⁷ is selected from the group H, halogen and C₁ -C₂ alkyl;

R⁸ is selected from the group H and C₁ -C₄ alkyl;

R¹¹, R¹² and R¹³ are independently selected from C₁ -C₂ alkyl;

R¹⁴ is selected form the group C₁ -C₄ alkyl, C₁ -C₄ alkoxy and phenyleach optionally substituted with 1 to 3 W; and

W is selected from the group halogen and C₁ -C₂ haloalkyl.

Preferred Compounds B are Compounds A wherein Q is Q-1.

Preferred Compounds C are Compounds A wherein Q is Q-2.

Preferred Compounds D are Compounds A wherein Q is Q-3.

Preferred Compounds E are Compounds A wherein Q is Q-4.

Preferred Compounds F are Compounds A wherein Q is Q-5.

Preferred Compounds G are Compounds A wherein Q is Q-6.

Preferred Compounds H are Compounds A wherein Q is Q-7.

Preferred Compounds I are Compounds A wherein Q is Q-8.

Specifically preferred for their biological activity and/or ease ofsynthesis are:

J. the compound of Preferred B which isβ-[(5-chloro-6-ethyl-4-pyrimidinyl)amino]-4-(1,1dimethylethyl)-benzeneethanol;

K. the compound of Preferred D which is5-chloro-6-ethyl-N-[2-[4-(trimethylsilyl)phenyl]ethyl]-4-pyrimidinamine;

L. the compound of Preferred E which is5-chloro-6-ethyl-N-[2-(2-naphthalenyl)ethyl]-4-pyrimidinamine

M. the compound of Preferred D which is5-chloro-6-ethyl-N-[1-[4-(trimethylsilyl)phenyl]ethyl]-4-pyrimidinamine;

N. the compound of Preferred B which isβ-[(5-chloro-6-ethyl-4-pyrimidinyl)amino]-4-(1,1-dimethymethyl)-benzenepropanol;

O. the compound of Preferred D which is5-chloro-6-ethyl-N-methyl-N-[2-[4-trimethylsilyl)phenyl]ethyl]-4-pyrimidinamine;and

P. the compound of Preferred D which is5-chloro-6-ethyl-N-[2-[3-(trimethylsilyl)phenyl]ethyl]-4-pyrimidinamine.

In the above recitations, the term "alkyl" used either alone or incompound word such as "alkylthio", "alkylene", or "haloalkyl", denotesstraight or branched alkyl, e.g., methyl, ethyl, n-propyl, isopropyl, orthe different butyl, pentyl or hexyl isomers.

Alkoxy denotes methoxy, ethoxy, n-propyloxy, isopropyloxy and thedifferent butoxy, pentoxy or hexyloxy isomers.

Alkenyl denotes straight or branched chain alkenes, e.g., vinyl,1-propenyl, 2-propenyl, 3-propenyl and the different butenyl, pentenyland hexenyl isomers. Alkynyl denotes straight chain or branched alkynes,e.g., ethynyl, 1-propynyl, 3-propynyl and the different butynyl,pentynyl and hexynyl isomers.

Alkylthio denotes methylthio, ethylthio and the different propylthio,butylthio, pentylthio and hexylthio isomers.

Alkylsulfinyl, alkylsulfonyl, alkylamino, etc., are defined analogouslyto the above examples.

Cycloalkyl denotes cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl.

The term "halogen", either alone or in compound words such as"haloalkyl", denotes fluorine, chlorine, bromine or iodine. Further,when used in compound words such as "haloalkyl" said alkyl may bepartially or fully substituted with halogen atoms, which may be the sameor different. Examples of haloalkyl include CH₂ CH₂ F, CF₂ CF₃ and CH₂CHFCl. The terms "halocycloalkyl", "haloalkenyl" and "haloalkynyl" aredefined analogously to the term "haloalkyl".

The total number of carbon atoms in a substituent group is indicated bythe "C_(i) -C_(j) " prefix where i and j are numbers from 1 to 8. Forexample, C₁ -C₃ alkylsulfonyl designates methylsulfonyl throughpropylsulfonyl; C₂ alkoxyalkoxy designates OCH₂ OCH₃ ; C₄ alkoxyalkoxydesignates the various isomers of an alkoxy group substituted with asecond alkoxy group containing a total of 4 carbon atoms, examplesincluding OCH₂ OCH₂ CH₂ CH₃ and OCH₂ CH₂ OCH₂ CH₃ ; C₂ cyanoalkyldesignates CH₂ CN and C₃ cyanoalkyl designates CH₂ CH₂ CN and CH(CN)CH₃; C₂ alkylcarbonyl would designates C(O)CH₃ and C₄ alkylcarbonylincludes C(O)CH₂ CH₂ CH₃ and C(O)CH(CH₃)₂ ; and as a final example, C₃alkoxycarbonylalkyl designates CH₂ CO₂ CH₃ and C₄ alkoxycarbonylalkylincludes CH₂ CH₂ CO₂ CH₃, CH₂ CO₂ CH₂ CH₃ and CH(CH₃)CO₂ CH₃.

DETAILS OF THE INVENTION

Compounds of Formula I can be prepared according to the reaction shownin Scheme 1. In this scheme, Z represents a displaceable group such as ahalogen atom, an alkylthio group, and an alkyl- or arylsulfonyloxygroup. ##STR7##

The reaction of pyrimidine II with amine III is best carried out in thepresence of an acid acceptor or base. The base can be, but is notlimited to, triethylamine, pyridine, sodium hydride, or potassiumcarbonate. The synthetic process can be carried out in the absence orpresence of a solvent. Suitable solvents include those that will notparticipate in the above reaction, for example, toluene, xylene,N,N-dimethylformamide, and N,N-dimethylacetamide. Preferred temperaturesfor this process are from about 20° C. to 200° C. with temperaturesbetween 80° C. and 150° C. being particularly preferred.

Compounds of Formula I where R⁵ is an alkyl or acyl group can be bestprepared by reacting an amine of Formula III where R⁵ is an alkyl oracyl group with a pyrimidine of Formula II. The amine of Formula IIIwhere R⁵ is alkyl or acyl can be prepared by acylating or alkylating anamine of Formula III, where R⁵ is equal to hydrogen, using conventionalmethods known to those skilled in the art.

Pyrimidines of Formula II can be prepared by a variety of literaturemethods. Some particularly efficient processes are described by Fosteret al. in Org. Syn., 1955, 35, 80 and Ube Industries in JP 58(83)222,070.

One particularly useful method for preparing some of the preferredcompounds of this invention where Q is equal to Q-1 to Q-4, Q-7 and Q-8is shown in Scheme 2. ##STR8##

Reduction of esters of Formula I with a reducing agent, for example,Lithium aluminum hydride, gives an alcohol of Formula I where A is equalto CHCH₂ OH. The reaction is best performed in an ether solvent thatdissolves the starting ester (tetrahydrofuran) and at reducedtemperatures (0° C.). Esters of Formula I where A is equal to CHCO₂ Mecan be prepared according to Scheme 1 using amines of Formula III whereA is equal to CHCO₂ Me. These reactions are usually performed in thepresence of triethylamine in dimethylformamide at about 100° C. Therequisite amine of Formula III can in turn be prepared by the process inScheme 3. ##STR9##

Hydrolysis of amine III where A is equal to CHCN with hydrogen chloridein methanol at the reflux temperature of the solvent proceeds to give anamine of Formula III where A is equal to CHCO₂ Me. Finally, amines ofFormula III where A is equal to CHCN can be synthesized from aldehydesof Formula IV according to the reaction in Scheme 4. ##STR10##

Treatment of aldehydes of Formula IV with trimethylsilyl cyanide in thepresence of zinc chloride in methylene chloride at ambient temperatureleads to an intermediate which when further treated with ammonia inmethanol at 40° C. gives the desired amino cyanide product. Aldehydes ofFormula IV are either known compounds or can be prepared by conventionalmethods known to one skilled in the art.

Related compounds of Formula I where A is equal to CH(CO₂ Me)CH₂ and Qis equal to Q-1 to Q-4, Q-7 and Q-8 can be prepared according to theprocedures of O'Donnell etal. in J. Org. Chem., 1982, 47, 2663 and Storketal. in J. Org. Chem., 1976, 41, 3491.

Another particularly useful method for preparing some of the preferredcompounds of this invention where Q is equal to Q-1 to Q-4, Q-7 and Q-8is shown in Scheme 5. ##STR11##

Amines of Formula III where A is equal to CH₂ CH₂ can be prepared byreduction of nitriles of Formula V using alane. In situ formation ofalane in ether and then treatment with nitrile V at 0° C. gives thedesired primary amines in high yields. Nitriles of Formula V can in turnbe synthesized by the displacement of a bromine atom from a bromide ofFormula VI with potassium cyanide (Scheme 6). ##STR12##

This reaction can be accomplished in refluxing ethanol and water ascosolvents. Bromides of Formula VI where Q is equal to Q-1 to Q-4, Q-7and Q-8 can be prepared according to the process shown in Scheme 7.##STR13##

Aryl methyl groups in compounds of Formula VII are subject to freeradical bromination by N-bromosuccinimide (NBS) in the presence oflight. The reaction is commonly done in refluxing carbon tetrachloridewith one equivalent of NBS. Compounds of Formula VII are eithercommercially available or can be prepared by conventional methods.Silylated compounds of Formula VII can be prepared according to themethods described by Habich et al. in Syn., 1979, 841. The germanylatedcompounds related to Formula VII can be made by simple modification ofthe procedure used for the silylated compounds that will be obvious toone skilled in the art.

Another particularly useful method for the preparation of some of thepreferred compounds of this invention where Q is equal to Q-1 to Q-4,Q-7 and Q-8 is shown in Scheme 8. ##STR14##

This process utilizes the method of Hart et al. described in J. Org.Chem., 1983, 48, 289. Amines of Formula III where A is equal to CHCH₂CH₃ are prepared from aldehydes of Formula IV by treatment with lithiumhexamethyldisilazide in THF at 0° C. followed by addition of ethylGrignard and refluxing. Some aldehydes of Formula IV where Q is equal toQ-1 to Q-4, Q-7 and Q-8 can be prepared by reaction of dibromides ofFormula VIII with silver nitrate in refluxing water/dimethoxyethanesolvent (Scheme 9). ##STR15##

The dibromides can, in turn, be prepared from compounds of Formula VIIwhere Q is equal to Q-1 to Q-4, Q-7 and Q-8. Aryl methyl compounds ofFormula VII are subject to free radical bromination with two equivalentsof NBS in the presence of light in refluxing carbon tetrachloride(Scheme 10). ##STR16##

The amines of Formula III prepared in Schemes 5 and can be used inScheme 1 to prepare preferred compounds of Formula I where Q is equal toQ-1 to Q-4, Q-7 and Q-8 of this invention.

Compounds of Formula I where Q is equal to Q-5 can be prepared accordingto Scheme 1 wherein the amine of Formula III is synthesized according tothe procedure of Henning et al. in J. Med. Chem., 1987, 30, 814.

Compounds of Formula I where Q is equal to Q-6 can be prepared accordingto Scheme 1 wherein the amine of Formula III is synthesized according tothe procedure of Gust et al., Tetrahedron, 1989, 45, 4867.

Compounds of Formula I where Q is equal to Q-2 and R¹ is equal to H canbe made by Friedel-Crafts reaction of pyrimidinylamines of Formula IXwith acid chlorides according to Scheme 11. ##STR17##

The pyrimidinylamines of Formula IX are known in the art (U.S. Pat. No.4,435,402) or can be made by methods disclosed in this application. Awide variety of solvents, acids and acid chlorides can be used in theFriedel-Crafts acylation of the compounds of Formula IX. TheFridel-Crafts acylation of aromatic compounds is well known to thoseskilled in the art and a listing of suitable solvents, acids andreactions conditions can be found in "Friedel-Crafts and RelatedReactions", Editor: George Olah, Interscience, New York 1964.Particularly suitable conditions for the instant invention are to use1,2-dichloroethane as a solvent with aluminum trichloride as the acid.The reaction is generally carried out under an inert atmosphere at thereflux temperature of the solvent with a slight excess of the acidchloride.

Compounds of Formula I where Q is equal to Q-2 and R¹⁴ is equal toalkoxy can be made by organometallic catalyzed carbonylation ofcompounds of Formula X according to Scheme 12. ##STR18##

The reaction can be carried out with a variety of alcohols XI. Palladiumcomplexes of triarylphosphines are the preferred catalysts in thisreaction. The catalyst is generally used at 1-10% of the substrateconcentration. Particularly preferred for its higher reactivity is thecomplex derived from palladium (II) acetate and bis(triphenylphosphinopropane). Use of this catalyst for the carbonylation of aryl triflatesand bromides has been reported by Dolle and Kruse Chem. Comm., 1987,904. The reaction can be carried out in a variety of solvents withdimethylsulfoxide being preferred for its higher catalyst turnoverratio. The temperature required for the reaction is determined by thenature of the catalyst and displaced halide or trillate. Generally thereaction is carried out at 70°-80° C. under a positive pressure ofcarbon monoxide. The presence of an acid scavenger is necessary for thereaction and a variety of inorganic and organic bases can serve thispurpose. Triethylamine is particularly suitable for the present case.

The following examples illustrate the invention.

EXAMPLE 1 Step A

α-amino-4-(1,1-dimethylethyl)benzeneacetonitrile, hydrochloride

Trimethylsilylcyanide (24 mL, 0.18 mole) was added dropwise to asolution of p-tert-butylbenzaldehyde (25 g, 0.15 mole) and zinc iodide(0.5g, 1.5 mole) in methylene chloride while maintaining a temperatureof 25° C. The yellow solution was stirred for 45 minutes and thenconcentrated to a viscous oil. The residue was treated with 250 mL ofammonia saturated methanol and heated at 40° C. for 1.5 hours.Concentration under vacuum gave a yellow solid which was dissolved in250 mL of ether and dried over solid MgSO₄. After filtration, hydrogenchloride gas was bubbled through the ether solution for about 5 minuteswhile maintaining a temperature of 20°-25° C. The solid product wasfiltered and washed with ether and then dried under vacuum to give 28.9g (86% yield), mp 190°-193° C.

¹ H NMR (Me₂ SO-d₆): δ 9.76 (s, 3H), 7.62, 7.54 (ABq, 4H), 5.94 (s, 1H),1.29 (s, 9H).

Step B

methyl α-amino-4-(1,1-dimethylethyl)benzeneacetate, hydrochloride

The product of Step A was dissolved in 40 mL of methanol and hydrogenchloride gas was bubbled into the solution while maintaining atemperature of 20°-30° C. The solution was refluxed for 2 hours, cooledto room temperature, and resaturated with HCl gas. After stirring atroom temperature overnight, the reaction mixture was concentrated undervacuum and the residue triturated with ether to give a white solid. Thesolid product was collected by filtration and dried under vacuum (34 g,99% yield), mp 185°-186° C.

¹ H NMR (Me₂ SO-d₆): δ 9.15 (s, 3H), 7.47 (s, 4H), 5.20 (s, 1H), 3.71(s, 3H), 1.28 (s, 9H).

Step C

methylα-[(5-chloro-6-ethyl-4-pyrimidinyl)aminol-4-(1,1-dimethylethyl)benzeneacetate

The ester from Step B (14.9 g, 58 mole) and4,5-dichloro-6-ethylpyrimidine (10.3 g, 58 mole) were dissolved in asolution of triethylamine (18 mL, 0.13 mole) and dimethylformamide (40mL) and heated at 100° C. for 6 hours. After cooling the solution wasdiluted with water and ether and partitioned. The aqueous phase wasextracted three times with ether and the combined organic phases werewashed two times with water, dried (MgSO₄) and concentrated. The cruderesidue was chromatographed on silica gel with 10% ethyl acetate/hexane.The resulting product was a waxy yellow solid (11.7 g, 56% yield).

¹ H NMR (CDCl₃): δ 8.40 (s, 1H), 7.39 (s, 4H), 6.23 (d, 1H), 5.72 (d,1H), 3.76 (s, 3H), 2.80 (q, 2H), 1.31 (s, 9H), 1.25 (t, 3H).

Step D

β-[(5-chloro-6-ethyl-4-pyrimidinyl)amino]-4-(1,1-dimethylethyl)benzeneethanol

The product of Step C (11.7 g, 32 mole) was dissolved in 80 mL oftetrahydrofuran and cooled to -5° C. with an ice/acetone bath. Lithiumaluminum hydride (1.2 g, 32 mole) was added portionwise over 15 minutesin such a manner as to control gas evolution and maintain thetemperature below 5° C. After complete addition of the LiAlH₄, thereaction was stirred at 0° C. for 30 minutes and then carefully quenchedby dropwise addition of saturated aqueous Na₂ SO₄ solution (10 mL). Themixture was diluted with ether and enough solid MgSO₄ was added to drythe suspension. Filtration and concentration of the ether solution gavea crude residue which was chromatographed on silica gel with 30% ethylacetate/hexane. The title compound was obtained as a waxy white solid(7.9 g, 68% yield), mp 117°-119° C.

¹ H NMR (CDCl₃): δ 8.39 (s, 1H), 7.39, 7.29 (ABq, 4H), 6.06 (d, 1H),5.25 (m, 1H), 4.01 (d, 2H), 2.80 (q, 2H), 1.32 (s, 9H), 1.26 (t, 3H).

EXAMPLE 2 Step A

2-naphthaleneethanamine

Aluminum trichloride (7.6 g, 57 mmole) was added in portions to 30 mL ofether cooled to 0° C. under nitrogen. In a separate flask, lithiumaluminum hydride (2.2 g, 57 mmole) was slurried in 30 mL of ether andcooled to -5° C. with an ice/acetone bath. The etherial aluminumtrichloride solution was added dropwise to the LiAlH₄ slurry at such arate as to maintain a temperature of 0° C. Fifteen minutes afteraddition was complete, 2-naphthylacetonitrile (4.0 g, 24 mmole) in 40 mLof ether was added dropwise while maintaining a temperature of 0° C. Thereaction mixture was stirred for an additional 15 minutes at 0° C. andthen allowed to warm to room temperature for 1 hour. After recooling to0° C., the reaction was quenched by careful dropwise addition of water.The mixture was diluted with ether, partitioned, and the aqueous phasewas basified with 30% NH₄ OH solution. Extraction of the aqueous phasewith ether, combination of the organic phases, drying, and concentrationgave a colorless oil (2.7g, 67% yield).

¹ H MNR (CDCl₃): δ 7.80 (m, 3H), 7.65 (s, 1H), 7.45 (m, 2H), 7.30 (m,1H), 3.06 (t, 2H), 2.91 (t, 2H), 1.35 (s, 2H).

Step B

5-chloro-6-ethyl-N-[2-(2-naphthalenyl)ethyl]-4-pyrimidinamine

The product of Step A (0.68 g, 4.0 mmole) and4,5-dichloro-6-ethylpyrimidine (0.71 g, 4.0 mmole) were dissolved intriethylamine (1.1 mL, 8.0 mmole) and toluene (7 mL) and heated toreflux for 4 hours. After cooling, the reaction mixture was treated with20 mL of water and 30 mL of ether, partitioned, and the aqueous phaseextracted with ether. The combined organic phases were dried (MgSO₄),concentrated and chromatographed on silica gel with 10% ethylacetate/hexane. The title compound was obtained as a white solid (0.77g, 62% yield) , mp 81°-83° C.

¹ H NMR (CDCl₃): δ 8.46 (s, 1H), 7.82 (m, 3H), 7.67 (s, 1H), 7.46 (m,3H), 5.50 (t, 1H), 3.85 (q, 2H), 3.09 (t, 2H), 2.78 (q, 2H), 1.25 (t,3H).

EXAMPLE 3 Step A

1-(dibromomethyl)-4-(trimethylsily)benzene

Trimethylsilyltoluene (5.0 g, 30 mmole), N-bromosuccinimide (11.4 g, 64mmole), and a catalytic amount of benzoyl peroxide were dissolved incarbon tetrachloride (300 mL) and heated to reflux under irradiation bya sunlamp. After 1 hour a solid had formed and the reaction wascomplete. The reaction mixture was filtered and concentrated to give thedesired product as a yellow liquid (10.7 g, 99% yield).

¹ H NMR (CDCl₃): δ 7.53 (s, 4H), 6.64 (s, 1H), 0.27 (s, 9H).

Step B

4-(trimethylsilyl)benzaldehyde

The product of Step A (10 g, 30 mmole) was dissolved in dimethoxyethane(160 mL) and heated to reflux. A solution of silver nitrate (15.3 g, 90mmole) in water (120 mL) was added dropwise while maintaining reflux.The reaction mixture was heated for 30 additional minutes and thencooled and the liquid decanted away from the percipitate. The solid wastriturated with ether and the combined organic phases were washed oncewith water, dried (MgSO₄), and concentrated to give the desired productas a pale yellow oil (6 g, 99% yield).

¹ H NMR (CDCl₃): δ 10.02 (s, 1H), 7.83, 7.70 (ABq, 4H), 0.31 (s, 9H).

Step C

α-ethyl-4-(trimethylsilyl)benzenemethanamine

To a solution of hexamethyldisilazane (4.3 mL, 20 mmole) intetrahydrofuran (5 mL) at 0° C. was added n-butyllithium (8.4 mL of2.5M, 21 mmole) dropwise. The mixture was allowed to warm to roomtemperature for 20 minutes and then recooled to 0° C. In a separateflask, the product of Step B (3.0 g, 17 mmole) in tetrahydrofuran (10mL) was cooled to 0° C. The lithiohexamethyldisilazane solution wasadded via cannula to the aldehyde solution. The reaction mixture waswarmed to 22° C. for 20 minutes and then ethyl magnesium bromide (14 mLof 3.0M, 42 mmole) was added dropwise. After heating the mixture atreflux for 12 hours, it was cooled and quenched with saturated aqueousammonium chloride solution. The aqueous phase was separated andextracted with ether. Combination of the organic phases, drying (MgSO₄),and concentration gave a crude residue which was chromatographed onsilica gel with ethyl acetate. The desired product was obtained as acolorless oil (0.95 g, 27% yield).

¹ H NMR (CDCl₃): δ 7.48, 7.31 (ABq, 4H), 3.79. (t, 1H), 1.70 (t, 2H),1.62 (s, 2H), 0.88 (t, 3H), 0.26 (s, 9H).

Step D

5-chloro-6-ethyl-N-[1-[4-(trimethylsilyl)phenyl]propyl]-4-pyrimidinamine

The amine of Step C (1.1 g, 5.3 mmole) was reacted as in Step B ofExample 2 to give the title compound as a viscous oil (0.70 g, 38%yield).

¹ H NMR (CDCl₃): δ 8.38 (s, 1H), 7.49, 7.32 (ABq, 4H), 5.65 (d, 1H),5.15 (q, 1H), 2.78 (q, 2H), 1.93 (m, 2H), 1.25 (t, 3H), 0.96 (t, 3H),0.26 (s, 9H).

EXAMPLE 4 Step A

1-ethyl-4-trimethylsilylbenzene

Magnesium(9.5 g, 0.39 mole) was suspended in THF (60 mL) at roomtemperature. A solution of 4-bromo-1-ethylbenzene (49 mL, 0.36 mole) in300 mL of THF was added dropwise at such a rate as to maintain thetemperature between 30° and 60° C. When the addition was complete thereaction mixture was stirred for an additional hour and then cooled to30° C. Trimethylsilyl chloride (49 mL, 0.39 mole) was added dropwise atsuch a rate as to maintain the temperature between 30° and 40° C. Thethin suspension was stirred overnight at room temperature. Saturatedaqueous NH₄ Cl was added and the reaction mixture partitioned. Theaqueous phase was extracted three times with ether, and the combinedorganic phases were dried (MgSO₄) and concentrated. The resultant oil(60 g, 93% yield) was used in the next step without furtherpurification.

¹ H NMR (CDCl₃): δ 7.43, 7.22 (ABq, 4H), 2.64 (q, 2H), 1.24 (t, 3H),0.25 (s, 9H).

Step B

1-bromo-1-[4-trimethylsilylphenyl]ethane

The product of Step A (59 g, 0.33 mole) was dissolved in carbontetrachloride (700 mL). To this solution was added N-bromosuccinimide(59 g, 0.33 mole) and benzoyl peroxide (ca. 200 rag) in one portion. Thereaction mixture was heated to reflux for 2.5 hours while beingirradiated with a 275 watt sunlamp. After cooling, the solid succinimidewas removed by filtration and the filtrate was washed with saturatedaqueous NaHSO₃. Drying (MgSO₄) and concentration gave an oil (77 g, 91%yield) which was used in the next step without further purification.

¹ H NMR (CDCl₃ : δ 7.48, 7.43 (ABq, 4H), 5.20 (q, 1H), 2.07 (d, 3H),0.26 (s, 9H).

Step C

1-[4-trimethylsilylphenyl]-1-N-phthalimidoethane

The product from Step B (77 g, 0.30 mole) and potassium phthalimide (58g, 0.31 mole) were dissolved in DMF (300 mL). The reaction mixture washeated to 80° C. for one hour and then concentrated under vacuum at 80°C. to remove most of the: DMF. The residue was taken up in water andextracted three times with ether. The combined organic phases werewashed two times with water, dried (MgSO₄) and concentrated to give anoil (91 g, 94% yield) which was used in the next step without furtherpurification.

¹ H NMR (CDCl₃): δ 7.80 (m, 2H), 7.69 (m, 2H), 7.49 (s, 4H), 5.57 (q,1H), 1.93 (d, 3H), 0.23 (s, 9H).

Step D

α-methyl-4-trimethylsilylbenzenemethanamine

The product of Step C (91 g, 0.28 mole) and hydrazine monohydrate (14mL, 0.29 mole) were dissolved in methanol (400 mL) and heated to refluxfor two hours. After cooling, the reaction mixture was poured into 6%aqueous K₂ CO₃ solution. The aqueous mixture was extracted three timeswith ether and the combined organic phases were dried (MgSO₄) andconcentrated to give an oil (49 g, 90% yield) which was used in the nextstep without further purification.

¹ H NMR (CDCl₃): δ 7.48, 7.35 (ABq, 4H), 4.10 (q, 1H), 1.65 (brs, 2H),1.39 (d, 3H), 0.26 (s, 9H).

Step E

5-chloro-6-ethyl-N-[1-[4-(trimethylsilyl)phenyl]ethyl]-4-pyrimidinamine

The product of Step D (17 g, 86 mole), 4,5-dichloro-6-ethylpyrimidine(15 g, 86 mole) and triethylamine (24 mL, 170 mole) were dissolved intoluene (65 mL). The reaction mixture was heated to reflux overnight andthen cooled. Ether and water were added and the mixture was partitioned.The aqueous phase was extracted two times with ether and the combinedorganic phases were dried (MgSO₄) and concentrated. The resultant solidwas recrystallized from acetonitrile to give the title compound as awhite solid (17 g, 60% yield), mp 79°-80° C.

¹ H NMR (CDCl₃): δ 8.40 (s, 1H), 7.51, 7.36 (ABq, 4H), 5.60 (brd, 1H),5.37 (q, 1H), 2.78 (q, 2H), 1.60 (d, 3H), 1.25 (t, 3H), 0.26 (s, 9H).

EXAMPLE 5 Step A

4-[2-(4-bromophenyl)ethylaminol-5-chloro-6-ethylpyrimidine

4-Bromophenethylamine (4.4 g), 4,5-dichloro-6-ethylpyrimidine (2.5 g)and triethylamine (4 ml) were dissolved in dimethylacetamide (15 ml) andheated to 100°-120° C. for 4.5 h. The cooled solution was added to water(70 ml). The reaction mixture was filtered and the solid was dried bydissolution in methylene chloride and addition of magnesium sulfate. Theresidue was purified by column chromatography on silica gel inhexanes/ethyl acetate (4:1) to provide the product (3.4 g) which wasused directly in the next step, mp 98°-99° C.

Step B

4-[2-[(5-chloro-6-ethyl-4-pyrimidinyl)amino]ethyl]benzoic acid, ethylester

The product from Step A (0.71 g) was dissolved in dimethylsulfoxide (6ml) and treated with palladium acetate (35 rag) , bis(diphenylphosphino)propane (70 mg), ethanol (4 ml) and triethylamine(0.5 ml). It was heated under an atmosphere of carbon monoxide to70°-80° C. and held there for 6 h. The mixture was then cooled andtreated with 30 ml of water. The solid formed was dissolved in methylenechloride and dried with magnesium sulfate. The residue waschromatographed on silica gel with hexanes/ethyl acetate (3:1) to givethe desired product (0.5 g) as a solid, mp 134°-135° C.

NMR (CDCl₃, 200 Mhz) 8.4 (1H, ArH), 8.0 (1H, ArH), 7.3 (2H, ArH), 5.4(NH), 4.4 (q, 2H, CH₂ O), 3.8 (m, 2H, CH₂), 2.99 (m, 2H, CH₂), 1.4 (t,3H, Me), 1.3 (t, 3H, Me).

EXAMPLE 6

(4-chlorophenyl)-4-[2-[(5-chloro-6-ethyl-4-pyrimidinyl)amino]ethyl]phenylmethanone

A solution of 5-chloro-6-ethyl-4-(2-phenethylamino)pyrimidine (0.84 g)in dichloroethane (15 ml) was treated with aluminum chloride (1.25 g).The mixture was treated with 4-chlorobenzoyl chloride (0.5 ml) andstirred for 1 h followed by heating at reflux for 1.5 h. The reactionmixture was cooled and treated with sodium hydroxide solution (20 ml,1N), and methylene chloride (15 ml). The layers were separated and theorganic layer was evaporated and the residue chromatographed on silicagel (hexanes/ethyl acetate 4:1) to give the product as an oil (0.72 g).

NMR (CDCl₃, 200 Mhz) 8.5 (1H, ArH), 7.7-7.3 (m, 8H, ArH), 5.6 (NH), 3.8(m, 2H, CH₂), 3.0 (m, 2H, CH₂), 2.8 (m, 2H, CH₂), 1.3 (m, 3H, Me).

By the general procedures described herein, or obvious modificationsthereof, the compounds of Index Tables A and B and Tables 1 through 9can be prepared.

                                      TABLE 1                                     __________________________________________________________________________     ##STR19##                                                                    R.sup.5  R.sup.6   R.sup.5  R.sup.6                                           __________________________________________________________________________    A = CHR.sup.1 ; R.sup.1 = CO.sub.2 Me                                                            A = CH(R.sup.1)CH.sub.2 ; R.sup.1 = CO.sub.2 Me            H        4-tBu     H        4-tBu                                             H        4-CH.sub.2 CH.sub.2 OEt                                                                 H        4-CH.sub.2 CH.sub.2 OEt                           H        4-OCH.sub.2 CH.sub.2 OEt                                                                H        4-OCH.sub.2 CH.sub.2 OEt                          H        4-OCH.sub.2 CF.sub.3                                                                    H        4-OCH.sub.2 CF.sub.3                              H        4-CO.sub.2 tBu                                                                          H        4-CO.sub.2 tBu                                    H        3-OPh     H        3-OPh                                             H        3-O(4-FPh)                                                                              H        3-O(4-FPh)                                        Me       4-tBu     Me       4-tBu                                             Me       4-CH.sub.2 CH.sub.2 OEt                                                                 Me       4-CH.sub.2 CH.sub.2 OEt                           Me       4-OCH.sub.2 CH.sub.2 OEt                                                                Me       4-OCH.sub.2 CH.sub. 2 OEt                         Me       4-OCH.sub.2 CF.sub.3                                                                    Me       4-OCH.sub.2 CF.sub.3                              Me       4-CO.sub.2 tBu                                                                          Me       4-CO.sub.2 tBu                                    Me       3-OPh     Me       3-OPh                                             Me       3-O(4-FPh)                                                                              Me       3-O(4-FPh)                                        C(O)imidazole                                                                          4-tBu     C(O)imidazole                                                                          4-tBu                                             C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                                                                 C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                           C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                                                                C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                          C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                                                                    C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                              C(O)imidazole                                                                          4-CO.sub.2 tBu                                                                          C(O)imidazole                                                                          4-CO.sub.2 tBu                                    C(O)imidazole                                                                          3-OPh     C(O)imidazole                                                                          3-OPh                                             C(O)imidazole                                                                          3-O(4-FPh)                                                                              C(O)imidazole                                                                          3-O(4-FPh)                                        SN(Me)CO.sub.2 Bu                                                                      4-tBu     SN(Me)CO.sub.2 Bu                                                                      4-tBu                                             SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                                                                 SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                           SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                                                                SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                          SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                                                                    SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                              SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                                                          SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                    SN(Me)CO.sub.2 Bu                                                                      3-OPh     SN(Me)CO.sub.2 Bu                                                                      3-OPh                                             SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                                                              SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                        A = CHR.sup.1 ; R.sup.1 = C(O)Me                                                                 A = CH(R.sup.1)CH.sub.2 ; R.sup.1 = C(O)Me                 H        4-tBu     H        4-tBu                                             H        4-CH.sub.2 CH.sub.2 OEt                                                                 H        4-CH.sub.2 CH.sub.2 OEt                           H        4-OCH.sub.2 CH.sub.2 OEt                                                                H        4-OCH.sub.2 CH.sub.2 OEt                          H        4-OCH.sub.2 CF.sub.3                                                                    H        4-OCH.sub.2 CF.sub.3                              H        4-CO.sub.2 tBu                                                                          H        4-CO.sub.2 tBu                                    H        3-OPh     H        3-OPh                                             H        3-O(4-FPh)                                                                              H        3-O(4-FPh)                                        Me       4-tBu     Me       4-tBu                                             Me       4-CH.sub.2 CH.sub.2 OEt                                                                 Me       4-CH.sub.2 CH.sub.2 OEt                           Me       4-OCH.sub.2 CH.sub.2 OEt                                                                Me       4-OCH.sub.2 CH.sub.2 OEt                          Me       4-OCH.sub.2 CF.sub.3                                                                    Me       4-OCH.sub.2 CF.sub.3                              Me       4-CO.sub.2 tBu                                                                          Me       4-CO.sub.2 tBu                                    Me       3-OPh     Me       3-OPh                                             Me       3-O(4-FPh)                                                                              Me       3-O(4-FPh)                                        C(O)imidazole                                                                          4-tBu     C(O)imidazole                                                                          4-tBu                                             C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                                                                 C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                           C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                                                                C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                          C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                                                                    C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                              C(O)imidazole                                                                          4-CO.sub.2 tBu                                                                          C(O)imidazole                                                                          4-CO.sub.2 tBu                                    C(O)imidazole                                                                          3-OPh     C(O)imidazole                                                                          3-OPh                                             C(O)imidazole                                                                          3-O(4-FPh)                                                                              C(O)imidazole                                                                          3-O(4-FPh)                                        SN(Me)CO.sub.2 Bu                                                                      4-tBu     SN(Me)CO.sub.2 Bu                                                                      4-tBu                                             SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                                                                 SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                           SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                                                                SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                          SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                                                                    SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                              SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                                                          SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                    SN(Me)CO.sub.2 Bu                                                                      3-OPh     SN(Me)CO.sub.2 Bu                                                                      3-OPh                                             SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                                                              SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                        A = CHR.sup.1 ; R.sup.1 = S(O)Me                                                                 A = CH(R.sup.1)CH.sub.2 ; R.sup.1 = S(O)Me                 H        4-tBu     H        4-tBu                                             H        4-CH.sub.2 CH.sub.2 OEt                                                                 H        4-CH.sub.2 CH.sub.2 OEt                           H        4-OCH.sub.2 CH.sub.2 OEt                                                                H        4-OCH.sub.2 CH.sub.2 OEt                          H        4-OCH.sub.2 CF.sub.3                                                                    H        4-OCH.sub.2 CF.sub.3                              H        4-CO.sub.2 tBu                                                                          H        4-CO.sub.2 tBu                                    H        3-OPh     H        3-OPh                                             H        3-O(4-FPh)                                                                              H        3-O(4-FPh)                                        Me       4-tBu     Me       4-tBu                                             Me       4-CH.sub.2 CH.sub.2 OEt                                                                 Me       4-CH.sub.2 CH.sub.2 OEt                           Me       4-OCH.sub.2 CH.sub.2 OEt                                                                Me       4-OCH.sub.2 CH.sub.2 OEt                          Me       4-OCH.sub.2 CF.sub.3                                                                    Me       4-OCH.sub.2 CF.sub.3                              Me       4-CO.sub.2 tBu                                                                          Me       4-CO.sub.2 tBu                                    Me       3-OPh     Me       3-OPh                                             Me       3-O(4-FPh)                                                                              Me       3-O(4-FPh)                                        C(O)imidazole                                                                          4-tBu     C(O)imidazole                                                                          4-tBu                                             C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                                                                 C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                           C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                                                                C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                          C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                                                                    C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                              C(O)imidazole                                                                          4-CO.sub.2 tBu                                                                          C(O)imidazole                                                                          4-CO.sub.2 tBu                                    C(O)imidazole                                                                          3-OPh     C(O)imidazole                                                                          3-OPh                                             C(O)imidazole                                                                          3-O(4-FPh)                                                                              C(O)imidazole                                                                          3-O(4-FPh)                                        SN(Me)CO.sub.2 Bu                                                                      4-tBu     SN(Me)CO.sub.2 Bu                                                                      4-tBu                                             SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                                                                 SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                           SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                                                                SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                          SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                                                                    SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                              SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                                                          SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                    SN(Me)CO.sub.2 Bu                                                                      3-OPh     SN(Me)CO.sub.2 Bu                                                                      3-OPh                                             SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                                                              SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                        A = CHR.sup.1 ; R.sup.1 = SCN                                                                    A = CH(R.sup.1)CH.sub.2 ; R.sup.1 = SCN                    H        4-tBu     H        4-tBu                                             H        4-CH.sub.2 CH.sub.2 OEt                                                                 H        4-CH.sub.2 CH.sub.2 OEt                           H        4-OCH.sub.2 CH.sub.2 OEt                                                                H        4-OCH.sub.2 CH.sub.2 OEt                          H        4-OCH.sub.2 CF.sub.3                                                                    H        4-OCH.sub.2 CF.sub.3                              H        4-CO.sub.2 tBu                                                                          H        4-CO.sub.2 tBu                                    H        3-OPh     H        3-OPh                                             H        3-O(4-FPh)                                                                              H        3-O(4-FPh)                                        Me       4-tBu     Me       4-tBu                                             Me       4-CH.sub.2 CH.sub.2 OEt                                                                 Me       4-CH.sub.2 CH.sub.2 OEt                           Me       4-OCH.sub.2 CH.sub.2 OEt                                                                Me       4-OCH.sub.2 CH.sub.2 OEt                          Me       4-OCH.sub.2 CF.sub.3                                                                    Me       4-OCH.sub.2 CF.sub.3                              Me       4-CO.sub.2 tBu                                                                          Me       4-CO.sub.2 tBu                                    Me       3-OPh     Me       3-OPh                                             Me       3-O(4-FPh)                                                                              Me       3-O(4-FPh)                                        C(O)imidazole                                                                          4-tBu     C(O)imidazole                                                                          4-tBu                                             C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                                                                 C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                           C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                                                                C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                          C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                                                                    C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                              C(O)imidazole                                                                          4-CO.sub.2 tBu                                                                          C(O)imidazole                                                                          4-CO.sub.2 tBu                                    C(O)imidazole                                                                          3-OPh     C(O)imidazole                                                                          3-OPh                                             C(O)imidazole                                                                          3-O(4-FPh)                                                                              C(O)imidazole                                                                          3-O(4-FPh)                                        SN(Me)CO.sub.2 Bu                                                                      4-tBu     SN(Me)CO.sub.2 Bu                                                                      4-tBu                                             SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                                                                 SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                           SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub. 2 CH.sub.2 OEt                                                               SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                          SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                                                                    SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                              SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                                                          SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                    SN(Me)CO.sub.2 Bu                                                                      3-OPh     SN(Me)CO.sub.2 Bu                                                                      3-OPh                                             SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                                                              SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                        A = CHR.sup.1 ; R.sup.1 = CN                                                                     A = CH(R.sup.1)CH.sub.2 ; R.sup.1 = CN                     H        4-tBu     H        4-tBu                                             H        4-CH.sub.2 CH.sub.2 OEt                                                                 H        4-CH.sub.2 CH.sub.2 OEt                           H        4-OCH.sub.2 CH.sub.2 OEt                                                                H        4-OCH.sub.2 CH.sub.2 OEt                          H        4-OCH.sub.2 CF.sub.3                                                                    H        4-OCH.sub.2 CF.sub.3                              H        4-CO.sub.2 tBu                                                                          H        4-CO.sub.2 tBu                                    H        3-OPh     H        3-OPh                                             H        3-O(4-FPh)                                                                              H        3-O(4-FPh)                                        Me       4-tBu     Me       4-tBu                                             Me       4-CH.sub.2 CH.sub.2 OEt                                                                 Me       4-CH.sub.2 CH.sub.2 OEt                           Me       4-OCH.sub.2 CH.sub.2 OEt                                                                Me       4-OCH.sub.2 CH.sub.2 OEt                          Me       4-OCH.sub.2 CF.sub.3                                                                    Me       4-OCH.sub.2 CF.sub.3                              Me       4-CO.sub.2 tBu                                                                          Me       4-CO.sub.2 tBu                                    Me       3-OPh     Me       3-OPh                                             Me       3-O(4-FPh)                                                                              Me       3-O(4-FPh)                                        C(O)imidazole                                                                          4-tBu     C(O)imidazole                                                                          4-tBu                                             C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                                                                 C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                           C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                                                                C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                          C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                                                                    C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                              C(O)imidazole                                                                          4-CO.sub.2 tBu                                                                          C(O)imidazole                                                                          4-CO.sub.2 tBu                                    C(O)imidazole                                                                          3-OPh     C(O)imidazole                                                                          3-OPh                                             C(O)imidazole                                                                          3-O(4-FPh)                                                                              C(O)imidazole                                                                          3-O(4-FPh)                                        SN(Me)CO.sub.2 Bu                                                                      4-tBu     SN(Me)CO.sub.2 Bu                                                                      4-tBu                                             SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                                                                 SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                           SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                                                                SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                          SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                                                                    SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                              SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                                                          SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                    SN(Me)CO.sub.2 Bu                                                                      3-OPh     SN(Me)CO.sub.2 Bu                                                                      3-OPh                                             SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                                                              SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                        A = CHR.sup.1 ; R.sup.1 = CH.sub.2 CN                                                            A = CH(R.sup.1)CH.sub.2 ; R.sup.1 = CH.sub.2 CN            H        4-tBu     H        4-tBu                                             H        4-CH.sub.2 CH.sub.2 OEt                                                                 H        4-CH.sub.2 CH.sub.2 OEt                           H        4-OCH.sub.2 CH.sub.2 OEt                                                                H        4-OCH.sub.2 CH.sub.2 OEt                          H        4-OCH.sub.2 CF.sub.3                                                                    H        4-OCH.sub.2 CF.sub.3                              H        4-CO.sub.2 tBu                                                                          H        4-CO.sub.2 tBu                                    H        3-OPh     H        3-OPh                                             H        3-O(4-FPh)                                                                              H        3-O(4-FPh)                                        Me       4-tBu     Me       4-tBu                                             Me       4-CH.sub.2 CH.sub.2 OEt                                                                 Me       4-CH.sub.2 CH.sub.2 OEt                           Me       4-OCH.sub.2 CH.sub.2 OEt                                                                Me       4-OCH.sub.2 CH.sub.2 OEt                          Me       4-OCH.sub.2 CF.sub.3                                                                    Me       4-OCH.sub.2 CF.sub.3                              Me       4-CO.sub.2 tBu                                                                          Me       4-CO.sub.2 tBu                                    Me       3-OPh     Me       3-OPh                                             Me       3-O(4-FPh)                                                                              Me       3-O(4-FPh)                                        C(O)imidazole                                                                          4-tBu     C(O)imidazole                                                                          4-tBu                                             C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                                                                 C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                           C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                                                                C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                          C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                                                                    C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                              C(O)imidazole                                                                          4-CO.sub.2 tBu                                                                          C(O)imidazole                                                                          4-CO.sub.2 tBu                                    C(O)imidazole                                                                          3-OPh     C(O)imidazole                                                                          3-OPh                                             C(O)imidazole                                                                          3-O(4-FPh)                                                                              C(O)imidazole                                                                          3-O(4-FPh)                                        SN(Me)CO.sub.2 Bu                                                                      4-tBu     SN(Me)CO.sub.2 Bu                                                                      4-tBu                                             SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                                                                 SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                           SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                                                                SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub. 2 CH.sub.2 OEt                         SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                                                                    SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                              SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                                                          SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                    SN(Me)CO.sub.2 Bu                                                                      3-OPh     SN(Me)CO.sub.2 Bu                                                                      3-OPh                                             SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                                                              SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                                           A = CH(R.sup.1)CH.sub.2 ;                                  A = CHR.sup.1 ; R.sup.1 = CH.sub.2 OC(Me).sub.2 OMe                                              R.sup.1 = CH.sub.2 OC(Me).sub.2 OMe                        H        4-tBu     H        4-tBu                                             H        4-CH.sub.2 CH.sub.2 OEt                                                                 H        4-CH.sub.2 CH.sub.2 OEt                           H        4-OCH.sub.2 CH.sub.2 OEt                                                                H        4-OCH.sub.2 CH.sub.2 OEt                          H        4-OCH.sub.2 CF.sub.3                                                                    H        4-OCH.sub.2 CF.sub.3                              H        4-CO.sub.2 tBu                                                                          H        4-CO.sub.2 tBu                                    H        3-OPh     H        3-OPh                                             H        3-O(4-FPh)                                                                              H        3-O(4-FPh)                                        Me       4-tBu     Me       4-tBu                                             Me       4-CH.sub.2 CH.sub.2 OEt                                                                 Me       4-CH.sub.2 CH.sub.2 OEt                           Me       4-OCH.sub.2 CH.sub.2 OEt                                                                Me       4-OCH.sub.2 CH.sub.2 OEt                          Me       4-OCH.sub.2 CF.sub.3                                                                    Me       4-OCH.sub.2 CF.sub.3                              Me       4-CO.sub.2 tBu                                                                          Me       4-CO.sub.2 tBu                                    Me       3-OPh     Me       3-OPh                                             Me       3-O(4-FPh)                                                                              Me       3-O(4-FPh)                                        C(O)imidazole                                                                          4-tBu     C(O)imidazole                                                                          4-tBu                                             C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                                                                 C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                           C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                                                                C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                          C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                                                                    C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                              C(O)imidazole                                                                          4-CO.sub.2 tBu                                                                          C(O)imidazole                                                                          4-CO.sub.2 tBu                                    C(O)imidazole                                                                          3-OPh     C(O)imidazole                                                                          3-OPh                                             C(O)imidazole                                                                          3-O(4-FPh)                                                                              C(O)imidazole                                                                          3-O(4-FPh)                                        SN(Me)CO.sub.2 Bu                                                                      4-tBu     SN(Me)CO.sub.2 Bu                                                                      4-tBu                                             SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                                                                 SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                           SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                                                                SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                          SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                                                                    SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                              SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                                                          SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                    SN(Me)CO.sub.2 Bu                                                                      3-OPh     SN(Me)CO.sub.2 Bu                                                                      3-OPh                                             SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                                                              SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                        A = CHR.sup.1 ; R.sup.1 = CH.sub.2 OH                                                            A = CH(R.sup.1)CH.sub.2 ; R.sup.1 = CH.sub.2 OH            H        4-tBu     H        4-tBu                                             H        4-CH.sub.2 CH.sub.2 OEt                                                                 H        4-CH.sub.2 CH.sub.2 OEt                           H        4-OCH.sub.2 CH.sub.2 OEt                                                                H        4-OCH.sub.2 CH.sub.2 OEt                          H        4-OCH.sub.2 CF.sub.3                                                                    H        4-OCH.sub.2 CF.sub.3                              H        4-CO.sub.2 tBu                                                                          H        4-CO.sub.2 tBu                                    H        3-OPh     H        3-OPh                                             H        3-O(4-FPh)                                                                              H        3-O(4-FPh)                                        Me       4-tBu     Me       4-tBu                                             Me       4-CH.sub.2 CH.sub.2 OEt                                                                 Me       4-CH.sub.2 CH.sub.2 OEt                           Me       4-OCH.sub.2 CH.sub.2 OEt                                                                Me       4-OCH.sub.2 CH.sub.2 OEt                          Me       4-OCH.sub.2 CF.sub.3                                                                    Me       4-OCH.sub.2 CF.sub.3                              Me       4-CO.sub.2 tBu                                                                          Me       4-CO.sub.2 tBu                                    Me       3-OPh     Me       3-OPh                                             Me       3-O(4-FPh)                                                                              Me       3-O(4-FPh)                                        C(O)imidazole                                                                          4-tBu     C(O)imidazole                                                                          4-tBu                                             C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                                                                 C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                           C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                                                                C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                          C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                                                                    C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                              C(O)imidazole                                                                          4-CO.sub.2 tBu                                                                          C(O)imidazole                                                                          4-CO.sub.2 tBu                                    C(O)imidazole                                                                          3-OPh     C(O)imidazole                                                                          3-OPh                                             C(O)imidazole                                                                          3-O(4-FPh)                                                                              C(O)imidazole                                                                          3-O(4-FPh)                                        SN(Me)CO.sub.2 Bu                                                                      4-tBu     SN(Me)CO.sub.2 Bu                                                                      4-tBu                                             SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                                                                 SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                           SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                                                                SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                          SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                                                                    SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                              SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                                                          SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                    SN(Me)CO.sub.2 Bu                                                                      3-OPh     SN(Me)CO.sub.2 Bu                                                                      3-OPh                                             SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                                                              SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                        A = CH.sub.2 CHR.sup.1 ; R.sup.1 = CH.sub.2 OH                                                   A = CH(R.sup.1)CH.sub.2 CH.sub.2 ; R.sup.1 = CH.sub.2                         OH                                                         H        4-tBu     H        4-tBu                                             H        4-CH.sub.2 CH.sub.2 OEt                                                                 H        4-CH.sub.2 CH.sub.2 OEt                           H        4-OCH.sub.2 CH.sub.2 OEt                                                                H        4-OCH.sub.2 CH.sub.2 OEt                          H        4-OCH.sub.2 CF.sub.3                                                                    H        4-OCH.sub.2 CF.sub.3                              H        4-CO.sub.2 tBu                                                                          H        4-CO.sub.2 tBu                                    H        3-OPh     H        3-OPh                                             H        3-O(4-FPh)                                                                              H        3-O(4-FPh)                                        Me       4-tBu     Me       4-tBu                                             Me       4-CH.sub.2 CH.sub.2 OEt                                                                 Me       4-CH.sub.2 CH.sub.2 OEt                           Me       4-OCH.sub.2 CH.sub.2 OEt                                                                Me       4-OCH.sub.2 CH.sub.2 OEt                          Me       4-OCH.sub.2 CF.sub.3                                                                    Me       4-OCH.sub.2 CF.sub.3                              Me       4-CO.sub.2 tBu                                                                          Me       4-CO.sub.2 tBu                                    Me       3-OPh     Me       3-OPh                                             Me       3-O(4-FPh)                                                                              Me       3-O(4-FPh)                                        C(O)imidazole                                                                          4-tBu     C(O)imidazole                                                                          4-tBu                                             C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                                                                 C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                           C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                                                                C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                          C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                                                                    C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                              C(O)imidazole                                                                          4-CO.sub.2 tBu                                                                          C(O)imidazole                                                                          4-CO.sub.2 tBu                                    C(O)imidazole                                                                          3-OPh     C(O)imidazole                                                                          3-OPh                                             C(O)imidazole                                                                          3-O(4-FPh)                                                                              C(O)imidazole                                                                          3-O(4-FPh)                                        SN(Me)CO.sub.2 Bu                                                                      4-tBu     SN(Me)CO.sub.2 Bu                                                                      4-tBu                                             SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                                                                 SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                           SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                                                                SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                          SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                                                                    SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                              SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                                                          SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                    SN(Me)CO.sub.2 Bu                                                                      3-OPh     SN(Me)CO.sub.2 Bu                                                                      3-OPh                                             SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                                                              SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                        A = CHR.sup.1 ; R.sup.1 = CH(Me)OH                                                               A = CH(R.sup.1)CH.sub.2 ; R.sup.1 = CH(Me)OH               H        4-tBu     H        4-tBu                                             H        4-CH.sub.2 CH.sub.2 OEt                                                                 H        4-CH.sub.2 CH.sub.2 OEt                           H        4-OCH.sub.2 CH.sub.2 OEt                                                                H        4-OCH.sub.2 CH.sub.2 OEt                          H        4-OCH.sub.2 CF.sub.3                                                                    H        4-OCH.sub.2 CF.sub.3                              H        4-CO.sub.2 tBu                                                                          H        4-CO.sub.2 tBu                                    H        3-OPh     H        3-OPh                                             H        3-O(4-FPh)                                                                              H        3-O(4-FPh)                                        Me       4-tBu     Me       4-tBu                                             Me       4-CH.sub.2 CH.sub.2 OEt                                                                 Me       4-CH.sub.2 CH.sub.2 OEt                           Me       4-OCH.sub.2 CH.sub.2 OEt                                                                Me       4-OCH.sub.2 CH.sub.2 OEt                          Me       4-OCH.sub.2 CF.sub.3                                                                    Me       4-OCH.sub.2 CF.sub.3                              Me       4-CO.sub.2 tBu                                                                          Me       4-CO.sub.2 tBu                                    Me       3-OPh     Me       3-OPh                                             Me       3-O(4-FPh)                                                                              Me       3-O(4-FPh)                                        C(O)imidazole                                                                          4-tBu     C(O)imidazole                                                                          4-tBu                                             C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                                                                 C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                           C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                                                                C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                          C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                                                                    C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                              C(O)imidazole                                                                          4-CO.sub.2 tBu                                                                          C(O)imidazole                                                                          4-CO.sub.2 tBu                                    C(O)imidazole                                                                          3-OPh     C(O)imidazole                                                                          3-OPh                                             C(O)imidazole                                                                          3-O(4-FPh)                                                                              C(O)imidazole                                                                          3-O(4-FPh)                                        SN(Me)CO.sub.2 Bu                                                                      4-tBu     SN(Me)CO.sub.2 Bu                                                                      4-tBu                                             SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                                                                 SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                           SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                                                                SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                          SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                                                                    SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                              SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                                                          SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                    SN(Me)CO.sub.2 Bu                                                                      3-OPh     SN(Me)CO.sub.2 Bu                                                                      3-OPh                                             SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                                                              SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                        A = CHR.sup.1 ; R.sup.1 = CH.sub.2 OCH.sub.2 CF.sub.3                                            A = CH(R.sup.1)CH.sub.2 ; R.sup.1 = CH.sub.2 OCH.sub.2                        CF.sub.3                                                   H        4-tBu     H        4-tBu                                             H        4-CH.sub.2 CH.sub.2 OEt                                                                 H        4-CH.sub.2 CH.sub.2 OEt                           H        4-OCH.sub.2 CH.sub.2 OEt                                                                H        4-OCH.sub.2 CH.sub.2 OEt                          H        4-OCH.sub.2 CF.sub.3                                                                    H        4-OCH.sub.2 CF.sub.3                              H        4-CO.sub.2 tBu                                                                          H        4-CO.sub.2 tBu                                    H        3-OPh     H        3-OPh                                             H        3-O(4-FPh)                                                                              H        3-O(4-FPh)                                        Me       4-tBu     Me       4-tBu                                             Me       4-CH.sub.2 CH.sub.2 OEt                                                                 Me       4-CH.sub.2 CH.sub.2 OEt                           Me       4-OCH.sub.2 CH.sub.2 OEt                                                                Me       4-OCH.sub.2 CH.sub.2 OEt                          Me       4-OCH.sub.2 CF.sub.3                                                                    Me       4-OCH.sub.2 CF.sub.3                              Me       4-CO.sub.2 tBu                                                                          Me       4-CO.sub.2 tBu                                    Me       3-OPh     Me       3-OPh                                             Me       3-O(4-FPh)                                                                              Me       3-O(4-FPh)                                        C(O)imidazole                                                                          4-tBu     C(O)imidazole                                                                          4-tBu                                             C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                                                                 C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                           C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                                                                C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                          C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                                                                    C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                              C(O)imidazole                                                                          4-CO.sub.2 tBu                                                                          C(O)imidazole                                                                          4-CO.sub.2 tBu                                    C(O)imidazole                                                                          3-OPh     C(O)imidazole                                                                          3-OPh                                             C(O)imidazole                                                                          3-O(4-FPh)                                                                              C(O)imidazole                                                                          3-O(4-FPh)                                        SN(Me)CO.sub.2 Bu                                                                      4-tBu     SN(Me)CO.sub.2 Bu                                                                      4-tBu                                             SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                                                                 SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                           SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                                                                SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                          SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                                                                    SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                              SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                                                          SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                    SN(Me)CO.sub.2 Bu                                                                      3-OPh     SN(Me)CO.sub.2 Bu                                                                      3-OPh                                             SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                                                              SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                        A = CHR.sup.1 ; R.sup.1 = CH.sub.2 NH.sub.2                                                      A = CH(R.sup.1)CH.sub.2 ; R.sup.1 = CH.sub.2 NH.sub.2      H        4-tBu     H        4-tBu                                             H        4-CH.sub.2 CH.sub.2 OEt                                                                 H        4-CH.sub.2 CH.sub.2 OEt                           H        4-OCH.sub.2 CH.sub.2 OEt                                                                H        4-OCH.sub.2 CH.sub.2 OEt                          H        4-OCH.sub.2 CF.sub.3                                                                    H        4-OCH.sub.2 CF.sub.3                              H        4-CO.sub.2 tBu                                                                          H        4-CO.sub.2 tBu                                    H        3-OPh     H        3-OPh                                             H        3-O(4-FPh)                                                                              H        3-O(4-FPh)                                        Me       4-tBu     Me       4-tBu                                             Me       4-CH.sub.2 CH.sub.2 OEt                                                                 Me       4-CH.sub.2 CH.sub.2 OEt                           Me       4-OCH.sub.2 CH.sub.2 OEt                                                                Me       4-OCH.sub.2 CH.sub.2 OEt                          Me       4-OCH.sub.2 CF.sub.3                                                                    Me       4-OCH.sub.2 CF.sub.3                              Me       4-CO.sub.2 tBu                                                                          Me       4-CO.sub.2 tBu                                    Me       3-OPh     Me       3-OPh                                             Me       3-O(4-FPh)                                                                              Me       3-O(4-FPh)                                        C(O)imidazole                                                                          4-tBu     C(O)imidazole                                                                          4-tBu                                             C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                                                                 C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                           C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                                                                C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                          C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                                                                    C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                              C(O)imidazole                                                                          4-CO.sub.2 tBu                                                                          C(O)imidazole                                                                          4-CO.sub.2 tBu                                    C(O)imidazole                                                                          3-OPh     C(O)imidazole                                                                          3-OPh                                             C(O)imidazole                                                                          3-O(4-FPh)                                                                              C(O)imidazole                                                                          3-O(4-FPh)                                        SN(Me)CO.sub.2 Bu                                                                      4-tBu     SN(Me)CO.sub.2 Bu                                                                      4-tBu                                             SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                                                                 SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                           SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                                                                SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                          SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                                                                    SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                              SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                                                          SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                    SN(Me)CO.sub.2 Bu                                                                      3-OPh     SN(Me)CO.sub.2 Bu                                                                      3-OPh                                             SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                                                              SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                        A = CHR.sup.1 ; R.sup.1 = CH.sub.2 OC(O)Me                                                       A = CH(R.sup.1)CH.sub.2 ; R.sup.1 = CH.sub.2 OC(O)Me       H        4-tBu     H        4-tBu                                             H        4-CH.sub.2 CH.sub.2 OEt                                                                 H        4-CH.sub.2 CH.sub.2 OEt                           H        4-OCH.sub.2 CH.sub.2 OEt                                                                H        4-OCH.sub.2 CH.sub.2 OEt                          H        4-OCH.sub.2 CF.sub.3                                                                    H        4-OCH.sub.2 CF.sub.3                              H        4-CO.sub.2 tBu                                                                          H        4-CO.sub.2 tBu                                    H        3-OPh     H        3-OPh                                             H        3-O(4-FPh)                                                                              H        3-O(4-FPh)                                        Me       4-tBu     Me       4-tBu                                             Me       4-CH.sub.2 CH.sub.2 OEt                                                                 Me       4-CH.sub.2 CH.sub.2 OEt                           Me       4-OCH.sub.2 CH.sub.2 OEt                                                                Me       4-OCH.sub.2 CH.sub.2 OEt                          Me       4-OCH.sub.2 CF.sub.3                                                                    Me       4-OCH.sub.2 CF.sub.3                              Me       4-CO.sub.2 tBu                                                                          Me       4-CO.sub.2 tBu                                    Me       3-OPh     Me       3-OPh                                             Me       3-O(4-F Ph)                                                                             Me       3-O(4-FPh)                                        C(O)imidazole                                                                          4-tBu     C(O)imidazole                                                                          4-tBu                                             C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                                                                 C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                           C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                                                                C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                          C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                                                                    C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                              C(O)imidazole                                                                          4-CO.sub.2 tBu                                                                          C(O)imidazole                                                                          4-CO.sub.2 tBu                                    C(O)imidazole                                                                          3-OPh     C(O)imidazole                                                                          3-OPh                                             C(O)imidazole                                                                          3-O(4-FPh)                                                                              C(O)imidazole                                                                          3-O(4-FPh)                                        SN(Me)CO.sub.2 Bu                                                                      4-tBu     SN(Me)CO.sub.2 Bu                                                                      4-tBu                                             SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                                                                 SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                           SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                                                                SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                          SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                                                                    SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                              SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                                                          SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                    SN(Me)CO.sub.2 Bu                                                                      3-OPh     SN(Me)CO.sub.2 Bu                                                                      3-OPh                                             SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                                                              SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                                           A = CH(R.sup.1)CH.sub.2 CH.sub.2 ;                         A = CH.sub.2 CHR.sup.1 ; R.sup.1 = CH.sub.2 OC(O)Me                                              R.sup.1 = CH.sub.2 OC(O)Me                                 H        4-tBu     H        4-tBu                                             H        4-CH.sub. 2 CH.sub.2 OEt                                                                H        4-CH.sub.2 CH.sub.2 OEt                           H        4-OCH.sub.2 CH.sub.2 OEt                                                                H        4-OCH.sub.2 CH.sub.2 OEt                          H        4-OCH.sub.2 CF.sub.3                                                                    H        4-OCH.sub.2 CF.sub.3                              H        4-CO.sub.2 tBu                                                                          H        4-CO.sub.2 tBu                                    H        3-OPh     H        3-OPh                                             H        3-O(4-FPh)                                                                              H        3-O(4-FPh)                                        Me       4-tBu     Me       4-tBu                                             Me       4-CH.sub.2 CH.sub.2 OEt                                                                 Me       4-CH.sub.2 CH.sub.2 OEt                           Me       4-OCH.sub.2 CH.sub.2 OEt                                                                Me       4-OCH.sub.2 CH.sub.2 OEt                          Me       4-OCH.sub.2 CF.sub.3                                                                    Me       4-OCH.sub.2 CF.sub.3                              Me       4-CO.sub.2 tBu                                                                          Me       4-CO.sub.2 tBu                                    Me       3-OPh     Me       3-OPh                                             Me       3-O(4-FPh)                                                                              Me       3-O(4-FPh)                                        C(O)imidazole                                                                          4-tBu     C(O)imidazole                                                                          4-tBu                                             C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                                                                 C(O)imidazole                                                                          4-CH.sub.2 CH.sub.2 OEt                           C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                                                                C(O)imidazole                                                                          4-OCH.sub.2 CH.sub.2 OEt                          C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                                                                    C(O)imidazole                                                                          4-OCH.sub.2 CF.sub.3                              C(O)imidazole                                                                          4-CO.sub.2 tBu                                                                          C(O)imidazole                                                                          4-CO.sub.2 tBu                                    C(O)imidazole                                                                          3-OPh     C(O)imidazole                                                                          3-OPh                                             C(O)imidazole                                                                          3-O(4-FPh)                                                                              C(O)imidazole                                                                          3-O(4-FPh)                                        SN(Me)CO.sub.2 Bu                                                                      4-tBu     SN(Me)CO.sub.2 Bu                                                                      4-tBu                                             SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                                                                 SN(Me)CO.sub.2 Bu                                                                      4-CH.sub.2 CH.sub.2 OEt                           SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                                                                SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CH.sub.2 OEt                          SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                                                                    SN(Me)CO.sub.2 Bu                                                                      4-OCH.sub.2 CF.sub.3                              SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                                                          SN(Me)CO.sub.2 Bu                                                                      4-CO.sub.2 tBu                                    SN(Me)CO.sub.2 Bu                                                                      3-OPh     SN(Me)CO.sub.2 Bu                                                                      3-OPh                                             SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                                                              SN(Me)CO.sub.2 Bu                                                                      3-O(4-FPh)                                        __________________________________________________________________________

                  TABLE 2                                                         ______________________________________                                         ##STR20##                                                                    ______________________________________                                        A          R.sup.5 A            R.sup.5                                       ______________________________________                                        R.sup.14 = OMe R.sup.14 = OMe                                                 CH.sub.2   H       CH.sub.2     C(O)imidazole                                 CH.sub.2 CH.sub.2                                                                        H       CH.sub.2 CH.sub.2                                                                          C(O)imidazole                                 CHMe       H       CHMe         C(O)imidazole                                 CHEt       H       CHEt         C(O)imidazole                                 CHiPr      H       CHiPr        C(O)imidazole                                 CH(Me)CH.sub.2                                                                           H       CH(Me)CH.sub.2                                                                             C(O)imidazole                                 CHCN       H       CHCN         C(O)imidazole                                 CHCH.sub.2 OH                                                                            H       CHCH.sub.2 OH                                                                              C(O)imidazole                                 CH(CH.sub.2 OH)CH.sub.2                                                                  H       CH(CH.sub.2 OH)CH.sub.2                                                                    C(O)imidazole                                 CH.sub.2   Me      CH.sub.2     SN(Me)CO.sub.2 Bu                             CH.sub.2 CH.sub.2                                                                        Me      CH.sub.2 CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                             CHMe       Me      CHMe         SN(Me)CO.sub.2 Bu                             CHEt       Me      CHEt         SN(Me)CO.sub.2 Bu                             CHiPr      Me      CHiPr        SN(Me)CO.sub.2 Bu                             CH(Me)CH.sub.2                                                                           Me      CH(Me)CH.sub.2                                                                             SN(Me)CO.sub.2 Bu                             CHCN       Me      CHCN         SN(Me)CO.sub.2 Bu                             CHCH.sub.2 OH                                                                            Me      CHCH.sub.2 OH                                                                              SN(Me)CO.sub.2 Bu                             CH(CH.sub.2 OH)CH.sub.2                                                                  Me      CH(CH.sub.2 OH)CH.sub.2                                                                    SN(Me)CO.sub.2 Bu                             R.sup.14 = OEt R.sup.14 = OEt                                                 CH.sub.2   H       CH.sub.2     C(O)imidazole                                 CH.sub.2 CH.sub.2                                                                        H       CH.sub.2 CH.sub.2                                                                          C(O)imidazole                                 CHMe       H       CHMe         C(O)imidazole                                 CHEt       H       CHEt         C(O)imidazole                                 CHiPr      H       CHiPr        C(O)imidazole                                 CH(Me)CH.sub.2                                                                           H       CH(Me)CH.sub.2                                                                             C(O)imidazole                                 CHCN       H       CHCN         C(O)imidazole                                 CHCH.sub.2 OH                                                                            H       CHCH.sub.2 OH                                                                              C(O)imidazole                                 CH(CH.sub.2 OH)CH.sub.2                                                                  H       CH(CH.sub.2 OH)CH.sub.2                                                                    C(O)imidazole                                 CH.sub.2   Me      CH.sub.2     SN(Me)CO.sub.2 Bu                             CH.sub.2 CH.sub.2                                                                        Me      CH.sub.2 CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                             CHMe       Me      CHMe         SN(Me)CO.sub.2 Bu                             CHEt       Me      CHEt         SN(Me)CO.sub.2 Bu                             CHiPr      Me      CHiPr        SN(Me)CO.sub.2 Bu                             CH(Me)CH.sub.2                                                                           Me      CH(Me)CH.sub.2                                                                             SN(Me)CO.sub.2 Bu                             CHCN       Me      CHCN         SN(Me)CO.sub.2 Bu                             CHCH.sub.2 OH                                                                            Me      CHCH.sub.2 OH                                                                              SN(Me)CO.sub.2 Bu                             CH(CH.sub.2 OH)CH.sub.2                                                                  Me      CH(CH.sub.2 OH)CH.sub.2                                                                    SN(Me)CO.sub.2 Bu                             R.sup.14 = OiPr                                                                              R.sup.14 = OiPr                                                CH.sub.2   H       CH.sub.2     C(O)imidazole                                 CH.sub.2 CH.sub. 2                                                                       H       CH.sub.2 CH.sub.2                                                                          C(O)imidazole                                 CHMe       H       CHMe         C(O)imidazole                                 CHEt       H       CHEt         C(O)imidazole                                 CHiPr      H       CHiPr        C(O)imidazole                                 CH(Me)CH.sub.2                                                                           H       CH(Me)CH.sub.2                                                                             C(O)imidazole                                 CHCN       H       CHCN         C(O)imidazole                                 CHCH.sub.2 OH                                                                            H       CHCH.sub.2 OH                                                                              C(O)imidazole                                 CH(CH.sub.2 OH)CH.sub.2                                                                  H       CH(CH.sub.2 OH)CH.sub.2                                                                    C(O)imidazole                                 CH.sub.2   Me      CH.sub.2     SN(Me)CO.sub.2 Bu                             CH.sub.2 CH.sub.2                                                                        Me      CH.sub.2 CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                             CHMe       Me      CHMe         SN(Me)CO.sub.2 Bu                             CHEt       Me      CHEt         SN(Me)CO.sub.2 Bu                             CHiPr      Me      CHiPr        SN(Me)CO.sub.2 Bu                             CH(Me)CH.sub.2                                                                           Me      CH(Me)CH.sub.2                                                                             SN(Me)CO.sub.2 Bu                             CHCN       Me      CHCN         SN(Me)CO.sub.2 Bu                             CHCH.sub.2 OH                                                                            Me      CHCH.sub.2 OH                                                                              SN(Me)CO.sub.2 Bu                             CH(CH.sub.2 OH)CH.sub.2                                                                  Me      CH(CH.sub.2 OH)CH.sub.2                                                                    SN(Me)CO.sub.2 Bu                             R.sup.14 = Et  R.sup.14 = Et                                                  CH.sub.2   H       CH.sub.2     C(O)imidazole                                 CH.sub.2 CH.sub.2                                                                        H       CH.sub.2 CH.sub.2                                                                          C(O)imidazole                                 CHMe       H       CHMe         C(O)imidazole                                 CHEt       H       CHEt         C(O)imidazole                                 CHiPr      H       CHiPr        C(O)imidazole                                 CH(Me)CH.sub.2                                                                           H       CH(Me)CH.sub.2                                                                             C(O)imidazole                                 CHCN       H       CHCN         C(O)imidazole                                 CHCH.sub.2 OH                                                                            H       CHCH.sub.2 OH                                                                              C(O)imidazole                                 CH(CH.sub.2 OH)CH.sub.2                                                                  H       CH(CH.sub.2 OH)CH.sub.2                                                                    C(O)imidazole                                 CH.sub.2   Me      CH.sub.2     SN(Me)CO.sub.2 Bu                             CH.sub.2 CH.sub.2                                                                        Me      CH.sub.2 CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                             CHMe       Me      CHMe         SN(Me)CO.sub.2 Bu                             CHEt       Me      CHEt         SN(Me)CO.sub.2 Bu                             CHiPr      Me      CHiPr        SN(Me)CO.sub.2 Bu                             CH(Me)CH.sub.2                                                                           Me      CH(Me)CH.sub.2                                                                             SN(Me)CO.sub.2 Bu                             CHCN       Me      CHCN         SN(Me)CO.sub.2 Bu                             CHCH.sub.2 OH                                                                            Me      CHCH.sub.2 OH                                                                              SN(Me)CO.sub.2 Bu                             CH(CH.sub.2 OH)CH.sub.2                                                                  Me      CH(CH.sub.2 OH)CH.sub.2                                                                    SN(Me)CO.sub.2 Bu                             R.sup.14 = Ph  R.sup.14 = Ph                                                  CH.sub.2   H       CH.sub.2     C(O)imidazole                                 CH.sub.2 CH.sub.2                                                                        H       CH.sub.2 CH.sub.2                                                                          C(O)imidazole                                 CHMe       H       CHMe         C(O)imidazole                                 CHEt       H       CHEt         C(O)imidazole                                 CHiPr      H       CHiPr        C(O)imidazole                                 CH(Me)CH.sub.2                                                                           H       CH(Me)CH.sub.2                                                                             C(O)imidazole                                 CHCN       H       CHCN         C(O)imidazole                                 CHCH.sub.2 OH                                                                            H       CHCH.sub.2 OH                                                                              C(O)imidazole                                 CH(CH.sub.2 OH)CH.sub.2                                                                  H       CH(CH.sub.2 OH)CH.sub.2                                                                    C(O)imidazole                                 CH.sub.2   Me      CH.sub.2     SN(Me)CO.sub.2 Bu                             CH.sub.2 CH.sub.2                                                                        Me      CH.sub.2 CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                             CHMe       Me      CHMe         SN(Me)CO.sub.2 Bu                             CHEt       Me      CHEt         SN(Me)CO.sub.2 Bu                             CHiPr      Me      CHiPr        SN(Me)CO.sub.2 Bu                             CH(Me)CH.sub.2                                                                           Me      CH(Me)CH.sub.2                                                                             SN(Me)CO.sub.2 Bu                             CHCN       Me      CHCN         SN(Me)CO.sub.2 Bu                             CHCH.sub.2 OH                                                                            Me      CHCH.sub.2 OH                                                                              SN(Me)CO.sub.2 Bu                             CH(CH.sub.2 OH)CH.sub.2                                                                  Me      CH(CH.sub.2 OH)CH.sub.2                                                                    SN(Me)CO.sub.2 Bu                             R.sup.14 = 4-FPh                                                                             R.sup.14 = 4-FPh                                               CH.sub.2   H       CH.sub.2     C(O)imidazole                                 CH.sub.2 CH.sub.2                                                                        H       CH.sub.2 CH.sub.2                                                                          C(O)imidazole                                 CHMe       H       CHMe         C(O)imidazole                                 CHEt       H       CHEt         C(O)imidazole                                 CHiPr      H       CHiPr        C(O)imidazole                                 CH(Me)CH.sub.2                                                                           H       CH(Me)CH.sub.2                                                                             C(O)imidazole                                 CHCN       H       CHCN         C(O)imidazole                                 CHCH.sub.2 OH                                                                            H       CHCH.sub.2 OH                                                                              C(O)imidazole                                 CH(CH.sub.2 OH)CH.sub.2                                                                  H       CH(CH.sub.2 OH)CH.sub.2                                                                    C(O)imidazole                                 CH.sub.2   Me      CH.sub.2     SN(Me)CO.sub.2 Bu                             CH.sub.2 CH.sub.2                                                                        Me      CH.sub.2 CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                             CHMe       Me      CHMe         SN(Me)CO.sub.2 Bu                             CHEt       Me      CHEt         SN(Me)CO.sub.2 Bu                             CHiPr      Me      CHiPr        SN(Me)CO.sub.2 Bu                             CH(Me)CH.sub.2                                                                           Me      CH(Me)CH.sub.2                                                                             SN(Me)CO.sub.2 Bu                             CHCN       Me      CHCN         SN(Me)CO.sub.2 Bu                             CHCH.sub.2 OH                                                                            Me      CHCH.sub.2 OH                                                                              SN(Me)CO.sub.2 Bu                             CH(CH.sub.2 OH)CH.sub.2                                                                  Me      CH(CH.sub.2 OH)CH.sub.2                                                                    SN(Me)CO.sub.2 Bu                             R.sup.14 = 4-ClPh                                                                            R.sup.14 = 4-ClPh                                               CH.sub.2  H       CH.sub.2     C(O)imidazole                                 CH.sub.2 CH.sub.2                                                                        H       CH.sub.2 CH.sub.2                                                                          C(O)imidazole                                 CHMe       H       CHMe         C(O)imidazole                                 CHEt       H       CHEt         C(O)imidazole                                 CHiPr      H       CHiPr        C(O)imidazole                                 CH(Me)CH.sub.2                                                                           H       CH(Me)CH.sub.2                                                                             C(O)imidazole                                 CHCN       H       CHCN         C(O)imidazole                                 CHCH.sub.2 OH                                                                            H       CHCH.sub.2 OH                                                                              C(O)imidazole                                 CH(CH.sub.2 OH)CH.sub.2                                                                  H       CH(CH.sub.2 OH)CH.sub.2                                                                    C(O)imidazole                                 CH.sub.2   Me      CH.sub.2     SN(Me)CO.sub.2 Bu                             CH.sub.2 CH.sub.2                                                                        Me      CH.sub.2 CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                             CHMe       Me      CHMe         SN(Me)CO.sub.2 Bu                             CHEt       Me      CHEt         SN(Me)CO.sub.2 Bu                             CHiPr      Me      CHiPr        SN(Me)CO.sub.2 Bu                             CH(Me)CH.sub.2                                                                           Me      CH(Me)CH.sub.2                                                                             SN(Me)CO.sub.2 Bu                             CHCN       Me      CHCN         SN(Me)CO.sub.2 Bu                             CHCH.sub.2 OH                                                                            Me      CHCH.sub.2 OH                                                                              SN(Me)CO.sub.2 Bu                             CH(CH.sub.2 OH)CH.sub.2                                                                  Me      CH(CH.sub.2 OH)CH.sub.2                                                                    SN(Me)CO.sub.2 Bu                             ______________________________________                                        R.sup.14           R.sup.14                                                   ______________________________________                                        R.sup.5 = H, A = CH.sub.2 CH.sub.2                                                               R.sup.5 = H, A = CH.sub.2 CH.sub.2                         Me                 2-F-phenyl                                                 i-Pr               3-F-phenyl                                                 c-Pr               2-Cl-phenyl                                                n-Bu               3-Cl-phenyl                                                i-Bu               2-CF.sub.3 -phenyl                                         t-Bu               3-CF.sub.3 -phenyl                                         c-Bu               4-CF.sub.3 -phenyl                                         n-amyl             4-Me-phenyl                                                i-amyl             4-OMe-phenyl                                               t-amyl             2,4-di-F-phenyl                                            cyclopentyl        3,4-di-F-phenyl                                            n-hexyl            3,5-di-F-phenyl                                            cyclohexyl         2,4-di-Cl-phenyl                                           OCH.sub.2 CF.sub.3 3,5-di-Cl-phenyl                                           On-Pr              3,4-di-Cl-phenyl                                           On-Bu                                                                         Oi-Bu                                                                         ______________________________________                                    

                  TABLE 3                                                         ______________________________________                                         ##STR21##                                                                    A                A                                                            ______________________________________                                        4-SiMe.sub.3 ; R.sup.5 = H; R.sup.13 = Me                                                      3-SiMe.sub.3 ; R.sup.5 = H; R.sup.13 = Me                    CH.sub.2         CH.sub.2                                                     CH.sub.2 CH.sub.2                                                                              CH.sub.2 CH.sub.2                                            CH.sub.2 CH.sub.2 CH.sub.2                                                                     CH.sub.2 CH.sub.2 CH.sub.2                                   CHMe             CHMe                                                         CHEt             CHEt                                                         CHiPr            CHiPr                                                        CH.sub.2 CHMe    CH.sub.2 CHMe                                                CH(Me)CH.sub.2   CH(Me)CH.sub.2                                               CH(Me)CH.sub.2 CH.sub.2                                                                        CH(Me)CH.sub.2 CH.sub.2                                      CH.sub.2 CH(Me)CH.sub.2                                                                        CH.sub.2 CH(Me)CH.sub.2                                      CMe.sub.2        CMe.sub.2                                                    CHCO.sub.2 Me    CHCO.sub.2 Me                                                CHC(O)Me         CHC(O)Me                                                     CHCN             CHCN                                                         CHCH.sub.2 OH    CHCH.sub.2 OH                                                CH(CH.sub.2 OH)CH.sub.2                                                                        CH(CH.sub.2 OH)CH.sub.2                                      4-SiMe.sub.3 ; R.sup.5 = Me; R.sup.13 = Me                                                     3-SiMe.sub.3 ; R.sup.5 = Me; R.sup.13 = Me                   CH.sub.2         CH.sub.2                                                     CH.sub.2 CH.sub.2                                                                              CH.sub.2 CH.sub.2                                            CH.sub.2 CH.sub.2 CH.sub.2                                                                     CH.sub.2 CH.sub.2 CH.sub.2                                   CHMe             CHMe                                                         CHEt             CHEt                                                         CHiPr            CHiPr                                                        CH.sub.2 CHMe    CH.sub.2 CHMe                                                CH(Me)CH.sub.2   CH(Me)CH.sub.2                                               CH(Me)CH.sub.2 CH.sub.2                                                                        CH(Me)CH.sub.2 CH.sub.2                                      CH.sub.2 CH(Me)CH.sub.2                                                                        CH.sub.2 CH(Me)CH.sub.2                                      CMe.sub.2        CMe.sub.2                                                    CHCO.sub.2 Me    CHCO.sub.2 Me                                                CHC(O)Me         CHC(O)Me                                                     CHCN             CHCN                                                         CHCH.sub.2 OH    CHCH.sub.2 OH                                                CH(CH.sub.2 OH)CH.sub.2                                                                        CH(CH.sub.2 OH)CH.sub.2                                      4-SiMe.sub.3 ; R.sup.5 = Et; R.sup.13 = Me                                                     3-SiMe.sub.3 ; R.sup.5 = Et; R.sup.13 = Me                   CH.sub.2         CH.sub.2                                                     CH.sub.2 CH.sub.2                                                                              CH.sub.2 CH.sub.2                                            CH.sub.2 CH.sub.2 CH.sub.2                                                                     CH.sub.2 CH.sub.2 CH.sub.2                                   CHMe             CHMe                                                         CHEt             CHEt                                                         CHiPr            CHiPr                                                        CH.sub.2 CHMe    CH.sub.2 CHMe                                                CH(Me)CH.sub.2   CH(Me)CH.sub.2                                               CH(Me)CH.sub.2 CH.sub.2                                                                        CH(Me)CH.sub.2 CH.sub.2                                      CH.sub.2 CH(Me)CH.sub.2                                                                        CH.sub.2 CH(Me)CH.sub.2                                      CMe.sub.2        CMe.sub.2                                                    CHCO.sub.2 Me    CHCO.sub.2 Me                                                CHC(O)Me         CHC(O)Me                                                     CHCN             CHCN                                                         CHCH.sub.2 OH    CHCH.sub.2 OH                                                CH(CH.sub.2 OH)CH.sub.2                                                                        CH(CH.sub.2 OH)CH.sub.2                                      4-SiMe.sub.3 ; R.sup.5 = C(O)imidazole;                                                        3-SiMe.sub.3 ; R.sup.5 = C(O)imidazole;                      R.sup.13 = Me    R.sup.13 = Me                                                CH.sub.2         CH.sub.2                                                     CH.sub.2 CH.sub.2                                                                              CH.sub.2 CH.sub.2                                            CH.sub.2 CH.sub.2 CH.sub.2                                                                     CH.sub.2 CH.sub.2 CH.sub.2                                   CHMe             CHMe                                                         CHEt             CHEt                                                         CHiPr            CHiPr                                                        CH.sub.2 CHMe    CH.sub.2 CHMe                                                CH(Me)CH.sub.2   CH(Me)CH.sub.2                                               CH(Me)CH.sub.2 CH.sub.2                                                                        CH(Me)CH.sub.2 CH.sub.2                                      CH.sub.2 CH(Me)CH.sub.2                                                                        CH.sub.2 CH(Me)CH.sub.2                                      CMe.sub.2        CMe.sub.2                                                    CHCO.sub.2 Me    CHCO.sub.2 Me                                                CHC(O)Me         CHC(O)Me                                                     CHCN             CHCN                                                         CHCH.sub.2 OH    CHCH.sub.2 OH                                                CH(CH.sub.2 OH)CH.sub.2                                                                        CH(CH.sub.2 OH)CH.sub.2                                      4-SiMe.sub.3 ; R.sup.5 = C(O)Me;                                                               3-SiMe.sub.3 ;                                               R.sup.13 = Me    R.sup.5 = C(O)Me; R.sup.13 = Me                              CH.sub.2         CH.sub.2                                                     CH.sub.2 CH.sub.2                                                                              CH.sub.2 CH.sub.2                                            CH.sub.2 CH.sub.2 CH.sub.2                                                                     CH.sub.2 CH.sub.2 CH.sub.2                                   CHMe             CHMe                                                         CHEt             CHEt                                                         CHiPr            CHiPr                                                        CH.sub.2 CHMe    CH.sub.2 CHMe                                                CH(Me)CH.sub.2   CH(Me)CH.sub.2                                               CH(Me)CH.sub.2 CH.sub.2                                                                        CH(Me)CH.sub.2 CH.sub.2                                      CH.sub.2 CH(Me)CH.sub.2                                                                        CH.sub.2 CH(Me)CH.sub.2                                      CMe.sub.2        CMe.sub.2                                                    CHCO.sub.2 Me    CHCO.sub.2 Me                                                CHC(O)Me         CHC(O)Me                                                     CHCN             CHCN                                                         CHCH.sub.2 OH    CHCH.sub.2 OH                                                CH(CH.sub.2 OH)CH.sub.2                                                                        CH(CH.sub.2 OH)CH.sub.2                                      4-SiMe.sub.3 ; R.sup.5 = CH.sub.2 CN;                                                          3-SiMe.sub.3 ;                                               R.sup.13 = Me    R.sup.5 = CH.sub.2 CN; R.sup.13 = Me                         CH.sub.2         CH.sub.2                                                     CH.sub.2 CH.sub.2                                                                              CH.sub.2 CH.sub.2                                            CH.sub.2 CH.sub.2 CH.sub.2                                                                     CH.sub.2 CH.sub.2 CH.sub.2                                   CHMe             CHMe                                                         CHEt             CHEt                                                         CHiPr            CHiPr                                                        CH.sub.2 CHMe    CH.sub.2 CHMe                                                CH(Me)CH.sub.2   CH(Me)CH.sub.2                                               CH(Me)CH.sub.2 CH.sub.2                                                                        CH(Me)CH.sub.2 CH.sub.2                                      CH.sub.2 CH(Me)CH.sub.2                                                                        CH.sub.2 CH(Me)CH.sub.2                                      CMe.sub.2        CMe.sub.2                                                    CHCO.sub.2 Me    CHCO.sub.2 Me                                                CHC(O)Me         CHC(O)Me                                                     CHCN             CHCN                                                         CHCH.sub.2 OH    CHCH.sub.2 OH                                                CH(CH.sub.2 OH)CH.sub.2                                                                        CH(CH.sub.2 OH)CH.sub.2                                      4-SiMe.sub.3 ; R.sup.5 = CH.sub.2 OEt;                                                         3-SiMe.sub.3 ;                                               R.sup.13 = Me    R.sup.5 =  CH.sub.2 OEt; R.sup.13 = Me                       CH.sub.2         CH.sub.2                                                     CH.sub.2 CH.sub.2                                                                              CH.sub.2 CH.sub.2                                            CH.sub.2 CH.sub.2 CH.sub.2                                                                     CH.sub.2 CH.sub.2 CH.sub.2                                   CHMe             CHMe                                                         CHEt             CHEt                                                         CHiPr            CHiPr                                                        CH.sub.2 CHMe    CH.sub.2 CHMe                                                CH(Me)CH.sub.2   CH(Me)CH.sub.2                                               CH(Me)CH.sub.2 CH.sub.2                                                                        CH(Me)CH.sub.2 CH.sub.2                                      CH.sub.2 CH(Me)CH.sub.2                                                                        CH.sub.2 CH(Me)CH.sub.2                                      CMe.sub.2        CMe.sub.2                                                    CHCO.sub.2 Me    CHCO.sub.2 Me                                                CHC(O)Me         CHC(O)Me                                                     CHCN             CHCN                                                         CHCH.sub.2 OH    CHCH.sub.2 OH                                                CH(CH.sub.2 OH)CH.sub.2                                                                        CH(CH.sub.2 OH)CH.sub.2                                      4-SiMe.sub.3 ; R.sup.5 = SNBu.sub.2 ;                                                          3-SiMe.sub.3 ;                                               R.sup.13 = Me    R.sup.5 = SNBu.sub.2 ; R.sup.13 = Me                         CH.sub.2         CH.sub.2                                                     CH.sub.2 CH.sub.2                                                                              CH.sub.2 CH.sub.2                                            CH.sub.2 CH.sub.2 CH.sub.2                                                                     CH.sub.2 CH.sub.2 CH.sub.2                                   CHMe             CHMe                                                         CHEt             CHEt                                                         CHiPr            CHiPr                                                        CH.sub.2 CHMe    CH.sub.2 CHMe                                                CH(Me)CH.sub.2   CH(Me)CH.sub.2                                               CH(Me)CH.sub.2 CH.sub.2                                                                        CH(Me)CH.sub.2 CH.sub.2                                      CH.sub.2 CH(Me)CH.sub.2                                                                        CH.sub.2 CH(Me)CH.sub.2                                      CMe.sub.2        CMe.sub.2                                                    CHCO.sub.2 Me    CHCO.sub.2 Me                                                CHC(O)Me         CHC(O)Me                                                     CHCN             CHCN                                                         CHCH.sub.2 OH    CHCH.sub.2 OH                                                CH(CH.sub.2 OH)CH.sub.2                                                                        CH(CH.sub.2 OH)CH.sub.2                                      4-SiMe.sub.3 ;                                                                R.sup.5 = SN(Me)CO.sub.2 Bu;                                                                   3-SiMe.sub.3 ; R.sup.5 = SN(Me)CO.sub.2 Bu;                  R.sup.13 = Me    R.sup.13 = Me                                                CH.sub.2         CH.sub.2                                                     CH.sub.2 CH.sub.2                                                                              CH.sub.2 CH.sub.2                                            CH.sub.2 CH.sub.2 CH.sub.2                                                                     CH.sub.2 CH.sub.2 CH.sub.2                                   CHMe             CHMe                                                         CHEt             CHEt                                                         CHiPr            CHiPr                                                        CH.sub.2 CHMe    CH.sub.2 CHMe                                                CH(Me)CH.sub.2   CH(Me)CH.sub.2                                               CH(Me)CH.sub.2 CH.sub.2                                                                        CH(Me)CH.sub.2 CH.sub.2                                      CH.sub.2 CH(Me)CH.sub.2                                                                        CH.sub.2 CH(Me)CH.sub.2                                      CMe.sub.2        CMe.sub.2                                                    CHCO.sub.2 Me    CHCO.sub.2 Me                                                CHC(O)Me         CHC(O)Me                                                     CHCN             CHCN                                                         CHCH.sub.2 OH    CHCH.sub.2 OH                                                CH(CH.sub.2 OH)CH.sub.2                                                                        CH(CH.sub.2 OH)CH.sub.2                                      4-SiMe.sub.2 R.sup.13 ; R.sup.5 = H;                                                           4-SiMe.sub.2 R.sup.13 ;                                      R.sup.13 = tBu   R.sup.5 = C(O)imidazole; R.sup.13 = tBu                      CH.sub.2         CH.sub.2                                                     CH.sub.2 CH.sub.2                                                                              CH.sub.2 CH.sub.2                                            CHMe             CHMe                                                         CHEt             CHEt                                                         CHiPr            CHiPr                                                        CH(Me)CH.sub.2   CH(Me)CH.sub.2                                               CHCH.sub.2 OH    CHCH.sub.2 OH                                                CH(CH.sub.2 OH)CH.sub.2                                                                        CH(CH.sub.2 OH)CH.sub.2                                      4-SiMe.sub.2 R.sup.13 ; R.sup.5 = Me;                                                          4-SiMe.sub.2 R.sup.13 ;                                      R.sup.13 = tBu   R.sup.5 = SN(Me)CO.sub.2 Bu; R.sup.13 = tBu                  CH.sub.2         CH.sub.2                                                     CH.sub.2 CH.sub.2                                                                              CH.sub.2 CH.sub.2                                            CHMe             CHMe                                                         CHEt             CHEt                                                         CHiPr            CHiPr                                                        CH(Me)CH.sub.2   CH(Me)CH.sub.2                                               CHCH.sub.2 OH    CHCH.sub.2 OH                                                CH(CH.sub.2 OH)CH.sub.2                                                                        CH(CH.sub.2 OH)CH.sub.2                                      4-SiMe.sub.2 R.sup.13 ; R.sup.5 = H;                                                           4-SiMe.sub.2 R.sup.13 ;                                      R.sup.13 = Ph    R.sup.5 = C(O)imidazole; R.sup.13 = Ph                       CH.sub.2         CH.sub.2                                                     CH.sub.2 CH.sub.2                                                                              CH.sub.2 CH.sub.2                                            CHMe             CHMe                                                         CHEt             CHEt                                                         CHiPr            CHiPr                                                        CH(Me)CH.sub.2   CH(Me)CH.sub.2                                               CHCH.sub.2 OH    CHCH.sub.2 OH                                                CH(CH.sub.2 OH)CH.sub.2                                                                        CH(CH.sub.2 OH)CH.sub.2                                      4-SiMe.sub.2 R.sup.13 ; R.sup.5 = Me;                                                          4-SiMe.sub.2 R.sup.13 ;                                      R.sup.13 = Ph    R.sup.5 = SN(Me)CO.sub.2 Bu; R.sup.13 = Ph                   CH.sub.2         CH.sub.2                                                     CH.sub.2 CH.sub.2                                                                              CH.sub.2 CH.sub.2                                            CHMe             CHMe                                                         CHEt             CHEt                                                         CHiPr            CHiPr                                                        CH(Me)CH.sub.2   CH(Me)CH.sub.2                                               CHCH.sub.2 OH    CHCH.sub.2 OH                                                CH(CH.sub.2 OH)CH.sub.2                                                                        CH(CH.sub.2 OH)CH.sub.2                                                       4-SiMe.sub.2 R.sup.13 ;                                      4-SiMe.sub.2 R.sup.13 ; R.sup.5 = H;                                                           R.sup.5 = C(O)imidazole;                                     R.sup.13 = CH.sub.2 OEt                                                                        R.sup.13 = CH.sub.2 OEt                                      CH.sub.2         CH.sub.2                                                     CH.sub.2 CH.sub.2                                                                              CH.sub.2 CH.sub.2                                            CHMe             CHMe                                                         CHEt             CHEt                                                         CHiPr            CHiPr                                                        CH(Me)CH.sub.2   CH(Me)CH.sub.2                                               CHCH.sub.2 OH    CHCH.sub.2 OH                                                CH(CH.sub.2 OH)CH.sub.2                                                                        CH(CH.sub.2 OH)CH.sub.2                                                       4-SiMe.sub.2 R.sup.13 ;                                      4-SiMe.sub.2 R.sup.13 ; R.sup.5 = Me;                                                          R.sup.5 = SN(Me)CO.sub.2 Bu;                                 R.sup.13 = CH.sub.2 OEt                                                                        R.sup.13 = CH.sub.2 OEt                                      CH.sub.2         CH.sub.2                                                     CH.sub.2 CH.sub.2                                                                              CH.sub.2 CH.sub.2                                            CHMe             CHMe                                                         CHEt             CHEt                                                         CHiPr            CHiPr                                                        CH(Me)CH.sub.2   CH(Me)CH.sub.2                                               CHCH.sub.2 OH    CHCH.sub.2 OH                                                CH(CH.sub.2 OH)CH.sub.2                                                                        CH(CH.sub.2 OH)CH.sub.2                                      ______________________________________                                    

                  TABLE 4                                                         ______________________________________                                         ##STR22##                                                                    A                 A                                                           ______________________________________                                        R.sup.5 = H; R.sup.6 = H                                                                        R.sup.5 = Me; R.sup.6 = H                                   CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CH.sub.2 CH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2                                  CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH.sub.2 CHMe     CH.sub.2 CHMe                                               CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CH(Me)CH.sub.2 CH.sub.2                                                                         CH(Me)CH.sub.2 CH.sub.2                                     CH.sub.2 CH(Me)CH.sub.2                                                                         CH.sub.2 CH(Me)CH.sub.2                                     CMe.sub.2         CMe.sub.2                                                   CHCO.sub.2 Me     CHCO.sub.2 Me                                               CHC(O)ME          CHC(O)Me                                                    CHCN              CHCN                                                        CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     R.sup.5  = Et; R.sup.6 = H                                                                      R.sup.5 = C(O)imidazole; R.sup.6 = H                        CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CH.sub.2 CH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2                                  CHMe              CHMe                                                        R.sup.5 = Et; R.sup.6 = H                                                                       R.sup.5 = C(O)imidazole; R.sup.6 = H                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH.sub.2 CHMe     CH.sub.2 CHMe                                               CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CH(Me)CH.sub.2 CH.sub.2                                                                         CH(Me)CH.sub.2 CH.sub.2                                     CH.sub.2 CH(Me)CH.sub.2                                                                         CH.sub.2 CH(Me)CH.sub.2                                     CMe.sub.2         CMe.sub.2                                                   CHCO.sub.2 Me     CHCO.sub.2 Me                                               CHC(O)Me          CHC(O)Me                                                    CHCN              CHCN                                                        CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     R.sup.5 = C(O)Me; R.sup.6 = H                                                                   R.sup.5 = CH.sub.2 CN; R.sup.6 = H                          CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CH.sub.2 CH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2                                  CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH.sub.2 CHMe     CH.sub.2 CHMe                                               CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CH(Me)CH.sub.2 CH.sub.2                                                                         CH(Me)CH.sub.2 CH.sub.2                                     CH.sub.2 CH(Me)CH.sub.2                                                                         CH.sub.2 CH(Me)CH.sub.2                                     CMe.sub.2         CMe.sub.2                                                   CHCO.sub.2 Me     CHCO.sub.2 Me                                               CHC(O)Me          CHC(O)Me                                                    CHCN              CHCN                                                        CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     R.sup.5 = CH.sub.2 OEt; R.sup.6 = H                                                             R.sup.5 = SNBu.sub.2 ; R.sup.6 = H                          CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CH.sub.2 CH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2                                  CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH.sub.2 CHMe     CH.sub.2 CHMe                                               CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CH(Me)CH.sub.2 CH.sub.2                                                                         CH(Me)CH.sub.2 CH.sub.2                                     CH.sub.2 CH(Me)CH.sub.2                                                                         CH.sub.2 CH(Me)CH.sub.2                                     CMe.sub.2         CMe.sub.2                                                   CHCO.sub.2 Me     CHCO.sub.2 Me                                               CHC(O)Me          CHC(O)Me                                                    CHCN              CHCN                                                        CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     R.sup.5 = SN(Me)CO.sub.2 Bu; R.sup.6 = H                                                        R.sup.5 = H; R.sup.6 = 6-Cl                                 CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CH.sub.2 CH.sub.2 CH.sub.2                                                                      CHMe                                                        CHMe              CHEt                                                        CHEt              CHiPr                                                       CHiPr             CH(Me)CH.sub.2                                                                CHCH.sub.2 OH                                                                 CH(CH.sub.2 OH)CH.sub.2                                     R.sup.5 = SN(Me)CO.sub.2 Bu; R.sup.6 = H                                                        R.sup.5 = H; R.sup.6 = 6-Cl                                 CH.sub.2 CHMe     CH.sub.2                                                    CH(Me)CH.sub.2    CH.sub.2 CH.sub.2                                           CH(Me)CH.sub.2 CH.sub.2                                                                         CHMe                                                        CH.sub.2 CH(Me)CH.sub.2                                                                         CHEt                                                        CMe.sub.2         CHiPr                                                       CHCO.sub.2 Me     CH(Me)CH.sub.2                                              CHC(O)Me          CHCH.sub.2 OH                                               CHCN              CH(CH.sub.2 OH)CH.sub.2                                     CHCH.sub.2 OH                                                                 CH(CH.sub.2 OH)CH.sub.2                                                       R.sup.5 = C(O)imidazole; R.sup.6 = 6-Cl                                                         R.sup.5 = H; R.sup.6 = 7-Cl                                 CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     R.sup.5 = SN(Me)CO.sub.2 Bu; R.sup.6 = 6-Cl                                                     R.sup.5 = Me; R.sup.6 = 7-Cl                                CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CHMe              CHMe                                                        R.sup. 5 = SN(Me)CO.sub.2 Bu; R.sup.6 = 6-Cl                                                    R.sup.5 = Me; R.sup.6 = 7-Cl                                CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     R.sup.5 = C(O)imidazole; R.sup.6 = 7-Cl                                                         R.sup.5 = H; R.sup.6 = 6-F                                  CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     R.sup.5 = SN(Me)CO.sub.2 Bu; R.sup.6 = 7-Cl                                                     R.sup.5 = Me; R.sup.6 = 6-F                                 CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     R.sup.5 = C(O)imidazole; R.sup.6 = 6-F                                                          R.sup.5 = H; R.sup.6 = 6-Me                                 CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     R.sup.5 = SN(Me)CO.sub.2 Bu; R.sup.6 = 6-F                                                      R.sup.5 = Me; R.sup.6 = 6-Me                                CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     R.sup.5 = C(O)imidazole; R.sup.6 = 6-Me                                                         R.sup.5 = H; R.sup.6 = 6-OMe                                CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CHMe              CHMe                                                        CHEt              CHEt                                                        R.sup.5 = C(O)imidazole; R.sup.6 = 6-Me                                                         R.sup.5 = H; R.sup.6 = 6-OMe                                CHiPr             CHiPr                                                       CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     R.sup.5 = SN(Me)CO.sub.2 Bu; R.sup.6  = 6-Me                                                    R.sup.5 = Me; R.sup.6 = 6-OMe                               CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     R.sup.5 = C(O)imidazole;                                                                        R.sup.5 = SN(Me)CO.sub.2 Bu;                                R.sup.6 = 6-OMe   R.sup.6 = 6-Me                                              CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     ______________________________________                                    

                  TABLE 5                                                         ______________________________________                                         ##STR23##                                                                    A        R.sup.6 = H  A          R.sup.6 = 6-Cl                               ______________________________________                                        R.sup.6 = H       R.sup.6 = 6-Cl                                              CH.sub.2 H            CH.sub.2   H                                            CHMe     H            CHMe       H                                            CHEt     H            CHEt       H                                            CHiPr    H            CHiPr      H                                            CHCN     H            CHCN       H                                            CHCH.sub.2 OH                                                                          H            CHCH.sub.2 OH                                                                            H                                            CH.sub.2 Me           CH.sub.2   Me                                           CHMe     Me           CHMe       Me                                           CHEt     Me           CHEt       Me                                           CHiPr    Me           CHiPr      Me                                           CHCN     Me           CHCN       Me                                           CHCH.sub.2 OH                                                                          Me           CHCH.sub.2 OH                                                                            Me                                           CH.sub.2 C(O)imidazole                                                                              CH.sub.2   C(O)imidazole                                CHMe     C(O)imidazole                                                                              CHMe       C(O)imidazole                                CHEt     C(O)imidazole                                                                              CHEt       C(O)imidazole                                CHiPr    C(O)imidazole                                                                              CHiPr      C(O)imidazole                                CHCN     C(O)imidazole                                                                              CHCN       C(O)imidazole                                CHCH.sub.2 OH                                                                          C(O)imidazole                                                                              CHCH.sub.2 OH                                                                            C(O)imidazole                                CH.sub.2 SN(Me)CO.sub.2 Bu                                                                          CH.sub.2   SN(Me)CO.sub.2 Bu                            CHMe     SN(Me)CO.sub.2 Bu                                                                          CHMe       SN(Me)CO.sub.2 Bu                            CHEt     SN(Me)CO.sub.2 Bu                                                                          CHEt       SN(Me)CO.sub.2 Bu                            CHiPr    SN(Me)CO.sub.2 Bu                                                                          CHiPr      SN(Me)CO.sub.2 Bu                            R.sup.6 = H       R.sup.6 = 6-Cl                                              CHCN     SN(Me)CO.sub.2 Bu                                                                          CHCN       SN(Me)CO.sub.2 Bu                            CHCH.sub.2 OH                                                                          SN(Me)CO.sub.2 Bu                                                                          CHCH.sub.2 OH                                                                            SN(Me)CO.sub.2 Bu                            R.sup.6 = 7-Cl    R.sup.6 = 6-F                                               CH.sub.2 H            CH.sub.2   H                                            CHMe     H            CHMe       H                                            CHEt     H            CHEt       H                                            CHiPr    H            CHiPr      H                                            CHCN     H            CHCN       H                                            CHCH.sub.2 OH                                                                          H            CHCH.sub.2 OH                                                                            H                                            CH.sub.2 Me           CH.sub.2   Me                                           CHMe     Me           CHMe       Me                                           CHEt     Me           CHEt       Me                                           CHiPr    Me           CHiPr      Me                                           CHCN     Me           CHCN       Me                                           CHCH.sub.2 OH                                                                          Me           CHCH.sub.2 OH                                                                            Me                                           CH.sub.2 C(O)imidazole                                                                              CH.sub.2   C(O)imidazole                                CHMe     C(O)imidazole                                                                              CHMe       C(O)imidazole                                CHEt     C(O)imidazole                                                                              CHEt       C(O)imidazole                                CHiPr    C(O)imidazole                                                                              CHiPr      C(O)imidazole                                CHCN     C(O)imidazole                                                                              CHCN       C(O)imidazole                                CHCH.sub.2 OH                                                                          C(O)imidazole                                                                              CHCH.sub.2 OH                                                                            C(O)imidazole                                CH.sub. 2                                                                              SN(Me)CO.sub.2 Bu                                                                          CH.sub.2   SN(Me)CO.sub.2 Bu                            CHMe     SN(Me)CO.sub.2 Bu                                                                          CHMe       SN(Me)CO.sub.2 Bu                            CHEt     SN(Me)CO.sub.2 Bu                                                                          CHEt       SN(Me)CO.sub.2 Bu                            CHiPr    SN(Me)CO.sub.2 Bu                                                                          CHiPr      SN(Me)CO.sub.2 Bu                            CHCN     SN(Me)CO.sub.2 Bu                                                                          CHCN       SN(Me)CO.sub.2 Bu                            CHCH.sub.2 OH                                                                          SN(Me)CO.sub.2 Bu                                                                          CHCH.sub.2 OH                                                                            SN(Me)CO.sub.2 Bu                            R.sup.6 = 6-Me    R.sup.6 = 6-OMe                                             CH.sub.2 H            CH.sub.2   H                                            CHMe     H            CHMe       H                                            CHEt     H            CHEt       H                                            CHiPr    H            CHiPr      H                                            CHCN     H            CHCN       H                                            CHCH.sub.2 OH                                                                          H            CHCH.sub.2 OH                                                                            H                                            CH.sub.2 Me           CH.sub.2   Me                                           CHMe     Me           CHMe       Me                                           CHEt     Me           CHEt       Me                                           CHiPr    Me           CHiPr      Me                                           CHCN     Me           CHCN       Me                                           CHCH.sub.2 OH                                                                          Me           CHCH.sub.2 OH                                                                            Me                                           CH.sub.2 C(O)imidazole                                                                              CH.sub.2   C(O)imidazole                                CHMe     C(O)imidazole                                                                              CHMe       C(O)imidazole                                CHEt     C(O)imidazole                                                                              CHEt       C(O)imidazole                                CHiPr    C(O)imidazole                                                                              CHiPr      C(O)imidazole                                CHCN     C(O)imidazole                                                                              CHCN       C(O)imidazole                                CHCH.sub.2 OH                                                                          C(O)imidazole                                                                              CHCH.sub.2 OH                                                                            C(O)imidazole                                CH.sub.2 SN(Me)CO.sub.2 Bu                                                                          CH.sub.2   SN(Me)CO.sub.2 Bu                            CHMe     SN(Me)CO.sub.2 Bu                                                                          CHMe       SN(Me)CO.sub.2 Bu                            CHEt     SN(Me)CO.sub.2 Bu                                                                          CHEt       SN(Me)CO.sub.2 Bu                            CHiPr    SN(Me)CO.sub.2 Bu                                                                          CHiPr      SN(Me)CO.sub.2 Bu                            CHCN     SN(Me)CO.sub.2 Bu                                                                          CHCN       SN(Me)CO.sub.2 Bu                            CHCH.sub.2 OH                                                                          SN(Me)CO.sub.2 Bu                                                                          CHCH.sub.2 OH                                                                            SN(Me)CO.sub.2 Bu                            ______________________________________                                    

                  TABLE 6                                                         ______________________________________                                         ##STR24##                                                                    A        R.sup.5      A          R.sup.5                                      ______________________________________                                        R.sup.6 = H       R.sup.6 = 6-Cl                                              CH.sub.2 H            CH.sub.2   H                                            CHMe     H            CHMe       H                                            CHEt     H            CHEt       H                                            CHiPr    H            CHiPr      H                                            CHCN     H            CHCN       H                                            CHCH.sub.2 OH                                                                          H            CHCH.sub.2 OH                                                                            H                                            CH.sub.2 Me           CH.sub.2   Me                                           CHMe     Me           CHMe       Me                                           CHEt     Me           CHEt       Me                                           CHiPr    Me           CHiPr      Me                                           CHCN     Me           CHCN       Me                                           CHCH.sub.2 OH                                                                          Me           CHCH.sub.2 OH                                                                            Me                                           CH.sub.2 C(O)imidazole                                                                              CH.sub.2   C(O)imidazole                                CHMe     C(O)imidazole                                                                              CHMe       C(O)imidazole                                CHEt     C(O)imidazole                                                                              CHEt       C(O)imidazole                                CHiPr    C(O)imidazole                                                                              CHiPr      C(O)imidazole                                CHCN     C(O)imidazole                                                                              CHCN       C(O)imidazole                                CHCH.sub.2 OH                                                                          C(O)imidazole                                                                              CHCH.sub.2 OH                                                                            C(O)imidazole                                CH.sub.2 SN(Me)CO.sub. 2 Bu                                                                         CH.sub.2   SN(Me)CO.sub.2 Bu                            CHMe     SN(Me)CO.sub.2 Bu                                                                          CHMe       SN(Me)CO.sub.2 Bu                            CHEt     SN(Me)CO.sub.2 Bu                                                                          CHEt       SN(Me)CO.sub.2 Bu                            CHiPr    SN(Me)CO.sub.2 Bu                                                                          CHiPr      SN(Me)CO.sub.2 Bu                            R.sup.6 = H       R.sup.6 = 6-Cl                                              CHCN     SN(Me)CO.sub.2 Bu                                                                          CHCN       SN(Me)CO.sub.2 Bu                            CHCH.sub.2 OH                                                                          SN(Me)CO.sub.2 Bu                                                                          CHCH.sub.2 OH                                                                            SN(Me)CO.sub.2 Bu                            R.sup.6 = 7-Cl    R.sup.6 = 6-F                                               CH.sub.2 H            CH.sub.2   H                                            CHMe     H            CHMe       H                                            CHEt     H            CHEt       H                                            CHiPr    H            CHiPr      H                                            CHCN     H            CHCN       H                                            CHCH.sub.2 OH                                                                          H            CHCH.sub.2 OH                                                                            H                                            CH.sub.2 Me           CH.sub.2   Me                                           CHMe     Me           CHMe       Me                                           CHEt     Me           CHEt       Me                                           CHiPr    Me           CHiPr      Me                                           CHCN     Me           CHCN       Me                                           CHCH.sub.2 OH                                                                          Me           CHCH.sub.2 OH                                                                            Me                                           CH.sub.2 C(O)imidazole                                                                              CH.sub.2   C(O)imidazole                                CHMe     C(O)imidazole                                                                              CHMe       C(O)imidazole                                CHEt     C(O)imidazole                                                                              CHEt       C(O)imidazole                                CHiPr    C(O)imidazole                                                                              CHiPr      C(O)imidazole                                CHCN     C(O)imidazole                                                                              CHCN       C(O)imidazole                                CHCH.sub.2 OH                                                                          C(O)imidazole                                                                              CHCH.sub.2 OH                                                                            C(O)imidazole                                CH.sub.2 SN(Me)CO.sub.2 Bu                                                                          CH.sub.2   SN(Me)CO.sub.2 Bu                            CHMe     SN(Me)CO.sub.2 Bu                                                                          CHMe       SN(Me)CO.sub.2 Bu                            CHEt     SN(Me)CO.sub.2 Bu                                                                          CHEt       SN(Me)CO.sub.2 Bu                            CHiPr    SN(Me)CO.sub.2 Bu                                                                          CHiPr      SN(Me)CO.sub.2 Bu                            CHCN     SN(Me)CO.sub.2 Bu                                                                          CHCN       SN(Me)CO.sub.2 Bu                            CHCH.sub.2 OH                                                                          SN(Me)CO.sub.2 Bu                                                                          CHCH.sub.2 OH                                                                            SN(Me)CO.sub.2 Bu                            R.sup.6 = Me      R.sup.6 = 6-OMe                                             CH.sub.2 H            CH.sub.2   H                                            CHMe     H            CHMe       H                                            CHEt     H            CHEt       H                                            CHiPr    H            CHiPr      H                                            CHCN     H            CHCN       H                                            CHCH.sub.2 OH                                                                          H            CHCH.sub.2 OH                                                                            H                                            CH.sub.2 Me           CH.sub.2   Me                                           CHMe     Me           CHMe       Me                                           CHEt     Me           CHEt       Me                                           CHiPr    Me           CHiPr      Me                                           CHCN     Me           CHCN       Me                                           CHCH.sub.2 OH                                                                          Me           CHCH.sub.2 OH                                                                            Me                                           CH.sub.2 C(O)imidazole                                                                              CH.sub.2   C(O)imidazole                                CHMe     C(O)imidazole                                                                              CHMe       C(O)imidazole                                CHEt     C(O)imidazole                                                                              CHEt       C(O)imidazole                                CHiPr    C(O)imidazole                                                                              CHiPr      C(O)imidazole                                CHCN     C(O)imidazole                                                                              CHCN       C(O)imidazole                                CHCH.sub.2 OH                                                                          C(O)imidazole                                                                              CHCH.sub.2 OH                                                                            C(O)imidazole                                CH.sub.2 SN(Me)CO.sub.2 Bu                                                                          CH.sub.2   SN(Me)CO.sub.2 Bu                            CHMe     SN(Me)CO.sub.2 Bu                                                                          CHMe       SN(Me)CO.sub.2 Bu                            CHEt     SN(Me)CO.sub.2 Bu                                                                          CHEt       SN(Me)CO.sub.2 Bu                            CHiPr    SN(Me)CO.sub.2 Bu                                                                          CHiPr      SN(Me)CO.sub.2 Bu                            CHCN     SN(Me)CO.sub.2 Bu                                                                          CHCN       SN(Me)CO.sub.2 Bu                            CHCH.sub.2 OH                                                                          SN(Me)CO.sub.2 Bu                                                                          CHCH.sub.2 OH                                                                            SN(Me)CO.sub.2 Bu                            ______________________________________                                    

                                      TABLE 7                                     __________________________________________________________________________     ##STR25##                                                                    __________________________________________________________________________    2-Q-7; G = O; R.sup.6 = H                                                                        2-Q-7; G = O; R.sup.6 = H                                  A         R.sup.5  A         R.sup.5                                          CH.sub.2  H        CH.sub.2  C(O)imidazole                                    CH.sub.2 CH.sub.2                                                                       H        CH.sub.2 CH.sub.2                                                                       C(O)imidazole                                    CHMe      H        CHHE      C(O)imidazole                                    CHEt      H        CHEt      C(O)imidazole                                    CHiPr     H        CHiPr     C(O)imidazole                                    CH(Me)CH.sub.2                                                                          H        CH(Me)CH.sub.2                                                                          C(O)imidazole                                    CHCN      H        CHCN      C(O)imidazole                                    CHCH.sub.2 OH                                                                           H        CHCH.sub.2 OH                                                                           C(O)imidazole                                    CH(CH.sub.2 OH)CH.sub.2                                                                 H        CH(CH.sub.2 OH)CH.sub.2                                                                 C(O)imidazole                                    CH.sub.2  Me       CH.sub.2  SN(Me)CO.sub.2 Bu                                CH.sub.2 CH.sub.2                                                                       Me       CH.sub.2 CH.sub.2                                                                       SN(Me)CO.sub.2 Bu                                CHMe      Me       CHMe      SN(Me)CO.sub. 2 Bu                               CHEt      Me       CHEt      SN(Me)CO.sub.2 Bu                                CHiPr     Me       CHiPr     SN(Me)CO.sub.2 Bu                                CH(Me)CH.sub.2                                                                          Me       CH(Me)CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                                CHCN      Me       CHCN      SN(Me)CO.sub.2 Bu                                CHCH.sub.2 OH                                                                           Me       CHCH.sub.2 OH                                                                           SN(Me)CO.sub.2 Bu                                CH(CH.sub.2 OH)CH.sub.2                                                                 Me       CH(CH.sub.2 OH)CH.sub.2                                                                 SN(Me)CO.sub.2 Bu                                2-Q-7; G = O; R.sup.6 = 6-Cl                                                                     2-Q-7; G = O; R.sup.6 = 6-Cl                               A         R.sup.5  A         R.sup.5                                          CH.sub.2  H        CH.sub.2  C(O)imidazole                                    CH.sub.2 CH.sub.2                                                                       H        CH.sub.2 CH.sub.2                                                                       C(O)imidazole                                    CHMe      H        CHMe      C(O)imidazole                                    2-Q-7; G = O; R.sup.6 = 6-Cl                                                                     2-Q-7; G = O; R.sup.6 = 6-Cl                               A         R.sup.5  A         R.sup.5                                          CHEt      H        CHEt      C(O)imidazole                                    CHiPr     H        CHiPr     C(O)imidazole                                    CH(Me)CH.sub.2                                                                          H        CH(Me)CH.sub.2                                                                          C(O)imidazole                                    CHCN      H        CHCN      C(O)imidazole                                    CHCH.sub.2 OH                                                                           H        CHCH.sub.2 OH                                                                           C(O)imidazole                                    CH(CH.sub.2 OH)CH.sub.2                                                                 H        CH(CH.sub.2 OH)CH.sub.2                                                                 C(O)imidazole                                    CH.sub.2  Me       CH.sub.2  SN(Me)CO.sub.2 Bu                                CH.sub.2 CH.sub.2                                                                       Me       CH.sub.2 CH.sub.2                                                                       SN(Me)CO.sub.2 Bu                                CHMe      Me       CHME      SN(Me)CO.sub.2 Bu                                CHEt      Me       CHEt      SN(Me)CO.sub.2 Bu                                CHiPr     Me       CHiPr     SN(Me)CO.sub.2 Bu                                CH(Me)CH.sub.2                                                                          Me       CH(Me)CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                                CHCN      Me       CHCN      SN(Me)CO.sub.2 Bu                                CHCH.sub.2 OH                                                                           Me       CHCH.sub.2 OH                                                                           SN(Me)CO.sub.2 Bu                                CH(CH.sub.2 OH)CH.sub.2                                                                 Me       CH(CH.sub.2 OH)CH.sub.2                                                                 SN(Me)CO.sub.2 Bu                                2-Q-7; G = O; R.sup.6 = 7-Cl                                                                     2-Q-7; G = O; R.sup.6 = 7-Cl                               A         R.sup.5  A         R.sup.5                                          CH.sub.2  H        CH.sub.2  C(O)imidazole                                    CH.sub.2 CH.sub.2                                                                       H        CH.sub.2 CH.sub.2                                                                       C(O)imidazole                                    CHMe      H        CHMe      C(O)imidazole                                    CHEt      H        CHEt      C(O)imidazole                                    CHiPr     H        CHiPr     C(O)imidazole                                    CH(Me)CH.sub.2                                                                          H        CH(Me)CH.sub.2                                                                          C(O)imidazole                                    CHCN      H        CHCN      C(O)imidazole                                    CHCH.sub.2 OH                                                                           H        CHCH.sub.2 OH                                                                           C(O)imidazole                                    2-Q-7; G = O; R.sup.6 = 7-Cl                                                                     2-Q-7; G = O; R.sup.6 = 7-Cl                               A         R.sup.5  A         R.sup.5                                          CH(CH.sub.2 OH)CH.sub.2                                                                 H        CH(CH.sub. 2 OH)CH.sub.2                                                                C(O)imidazole                                    CH.sub.2  Me       CH.sub.2  SN(Me)CO.sub.2 Bu                                CH.sub.2 CH.sub.2                                                                       Me       CH.sub.2 CH.sub.2                                                                       SN(Me)CO.sub.2 Bu                                CHMe      Me       CHMe      SN(Me)CO.sub.2 Bu                                CHEt      Me       CHEt      SN(Me)CO.sub.2 Bu                                CHiPr     Me       CHiPr     SN(Me)CO.sub.2 Bu                                CH(Me)CH.sub.2                                                                          Me       CH(Me)CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                                CHCN      Me       CHCN      SN(Me)CO.sub.2 Bu                                CHCH.sub.2 OH                                                                           Me       CHCH.sub.2 OH                                                                           SN(Me)CO.sub.2 Bu                                CH(CH.sub.2 OH)CH.sub.2                                                                 Me       CH(CH.sub.2 OH)CH.sub.2                                                                 SN(Me)CO.sub.2 Bu                                3-Q-7; G = O; R.sup.6 = H                                                                        3-Q-7; G = O; R.sup.6 = H                                  A         R.sup.5  A         R.sup.5                                          CH.sub.2  H        CH.sub.2  C(O)imidazole                                    CH.sub.2 CH.sub.2                                                                       H        CH.sub.2 CH.sub.2                                                                       C(O)imidazole                                    CHMe      H        CHMe      C(O)imidazole                                    CHEt      H        CHEt      C(O)imidazole                                    CHiPr     H        CHiPr     C(O)imidazole                                    CH(Me)CH.sub.2                                                                          H        CH(Me)CH.sub.2                                                                          C(O)imidazole                                    CHCN      H        CHCN      C(O)imidazole                                    CHCH.sub.2 OH                                                                           H        CHCH.sub.2 OH                                                                           C(O)imidazole                                    CH(CH.sub.2 OH)CH.sub.2                                                                 H        CH(CH.sub.2 OH)CH.sub.2                                                                 C(O)imidazole                                    CH.sub.2  Me       CH.sub.2  SN(Me)CO.sub.2 Bu                                CH.sub.2 CH.sub.2                                                                       Me       CH.sub.2 CH.sub.2                                                                       SN(Me)CO.sub.2 Bu                                CHMe      Me       CHMe      SN(Me)CO.sub. 2 Bu                               CHEt      Me       CHEt      SN(Me)CO.sub.2 Bu                                CHiPr     Me       CHiPr     SN(Me)CO.sub.2 Bu                                CH(Me)CH.sub.2                                                                          Me       CH(Me)CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                                CHCN      Me       CHCN      SN(Me)CO.sub.2 Bu                                CHCH.sub.2 OH                                                                           Me       CHCH.sub.2 OH                                                                           SN(Me)CO.sub.2 Bu                                CH(CH.sub.2 OH)CH.sub.2                                                                 Me       CH(CH.sub.2 OH)CH.sub.2                                                                 SN(Me)CO.sub.2 Bu                                3-Q-7; G = O; R.sup.6 = 6-Cl                                                                     3-Q-7; G = O; R.sup.6 = 6-Cl                               A         R.sup.5  A         R.sup.5                                          CH.sub.2  H        CH.sub.2  C(O)imidazole                                    CH.sub.2 CH.sub.2                                                                       H        CH.sub.2 CH.sub.2                                                                       C(O)imidazole                                    CHMe      H        CHMe      C(O)imidazole                                    CHEt      H        CHEt      C(O)imidazole                                    CHiPr     H        CHiPr     C(O)imidazole                                    CH(Me)CH.sub.2                                                                          H        CH(Me)CH.sub.2                                                                          C(O)imidazole                                    CHCN      H        CHCN      C(O)imidazole                                    CHCH.sub.2 OH                                                                           H        CHCH.sub.2 OH                                                                           C(O)imidazole                                    CH(CH.sub.2 OH)CH.sub.2                                                                 H        CH(CH.sub.2 OH)CH.sub.2                                                                 C(O)imidazole                                    CH.sub.2  Me       CH.sub.2  SN(Me)CO.sub.2 Bu                                CH.sub.2 CH.sub.2                                                                       Me       CH.sub.2 CH.sub.2                                                                       SN(Me)CO.sub.2 Bu                                CHMe      Me       CHMe      SN(Me)CO.sub.2 Bu                                CHEt      Me       CHEt      SN(Me)CO.sub.2 Bu                                CHiPr     Me       CHiPr     SN(Me)CO.sub.2 Bu                                CH(Me)CH.sub.2                                                                          Me       CH(Me)CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                                CHCN      Me       CHCN      SN(Me)CO.sub.2 Bu                                CHCH.sub.2 OH                                                                           Me       CHCH.sub.2 OH                                                                           SN(Me)CO.sub.2 Bu                                CH(CH.sub.2 OH)CH.sub.2                                                                 Me       CH(CH.sub.2 OH)CH.sub.2                                                                 SN(Me)CO.sub.2 Bu                                3-Q-7; G = O; R.sup.6 = 7-Cl                                                                     3-Q-7; G = O; R.sup.6 = 7-Cl                               A         R.sup.5  A         R.sup.5                                          CH.sub.2  H        CH.sub.2  C(O)imidazole                                    CH.sub.2 CH.sub.2                                                                       H        CH.sub.2 CH.sub.2                                                                       C(O)imidazole                                    CHMe      H        CHMe      C(O)imidazole                                    CHEt      H        CHEt      C(O)imidazole                                    3-Q-7; G = O; R.sup.6 = 7-Cl                                                                     3-Q-7; G = O; R.sup.6 = 7-Cl                               A         R.sup.5  A         R.sup.5                                          CHiPr     H        CHiPr     C(O)imidazole                                    CH(Me)CH.sub.2                                                                          H        CH(Me)CH.sub.2                                                                          C(O)imidazole                                    CHCN      H        CHCN      C(O)imidazole                                    CHCH.sub.2 OH                                                                           H        CHCH.sub.2 OH                                                                           C(O)imidazole                                    CH(CH.sub.2 OH)CH.sub.2                                                                 H        CH(CH.sub.2 OH)CH.sub.2                                                                 C(O)imidazole                                    CH.sub.2  Me       CH.sub.2  SN(Me)CO.sub.2 Bu                                CH.sub.2 CH.sub.2                                                                       Me       CH.sub.2 CH.sub.2                                                                       SN(Me)CO.sub.2 Bu                                CHMe      Me       CHMe      SN(Me)CO.sub.2 Bu                                CHEt      Me       CHEt      SN(Me)CO.sub.2 Bu                                CHiPr     Me       CHiPr     SN(Me)CO.sub.2 Bu                                CH(Me)CH.sub.2                                                                          Me       CH(Me)CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                                CHCN      Me       CHCN      SN(Me)CO.sub.2 Bu                                CHCH.sub.2 OH                                                                           Me       CHCH.sub.2 OH                                                                           SN(Me)CO.sub.2 Bu                                CH(CH.sub.2 OH)CH.sub.2                                                                 Me       CH(CH.sub.2 OH)CH.sub.2                                                                 SN(Me)CO.sub.2 Bu                                2-Q-7; G = S; R.sup.6 = H                                                                        2-Q-7; G = S; R.sup.6 = H                                  A         R.sup.5  A         R.sup.5                                          CH.sub.2  H        CH.sub.2  SN(Me)CO.sub.2 Bu                                CH.sub.2 CH.sub.2                                                                       H        CH.sub.2 CH.sub.2                                                                       SN(Me)CO.sub.2 Bu                                CHMe      H        CHMe      SN(Me)CO.sub.2 Bu                                CHEt      H        CHEt      SN(Me)CO.sub.2 Bu                                CHiPr     H        CHiPr     SN(Me)CO.sub.2 Bu                                CH(Me)CH.sub.2                                                                          H        CH(Me)CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                                CHCN      H        CHCN      SN(Me)CO.sub.2 Bu                                CHCH.sub.2 OH                                                                           H        CHCH.sub.2 OH                                                                           SN(Me)CO.sub.2 Bu                                CH(CH.sub.2 OH)CH.sub.2                                                                 H        CH(CH.sub.2 OH)CH.sub.2                                                                 SN(Me)CO.sub.2 Bu                                CH.sub.2  Me       CH.sub.2  Et                                               CH.sub.2 CH.sub.2                                                                       Me       CH.sub.2 CH.sub.2                                                                       Et                                               2-Q-7; G = S; R.sup.6 = H                                                                        2-Q-7; G = S; R.sup.6 = H                                  A          R.sup.5 A         R.sup.5                                          CHMe      Me       CHMe      Et                                               CHEt      Me       CHEt      Et                                               CHiPr     Me       CHiPr     Et                                               CH(Me)CH.sub.2                                                                          Me       CH(Me)CH.sub.2                                                                          Et                                               CHCN      Me       CHCN      Et                                               CHCH.sub.2 OH                                                                           Me       CHCH.sub.2 OH                                                                           Et                                               CH(CH.sub.2 OH)CH.sub.2                                                                 Me       CH(CH.sub.2 OH)CH.sub.2                                                                 Et                                               CH.sub.2  C(O)imidazole                                                                          CH.sub.2  C(O)Me                                           CH.sub.2 CH.sub.2                                                                       C(O)imidazole                                                                          CH.sub.2 CH.sub.2                                                                       C(O)Me                                           CHMe      C(O)imidazole                                                                          CHMe      C(O)Me                                           CHEt      C(O)imidazole                                                                          CHEt      C(O)Me                                           CHiPr     C(O)imidazole                                                                          CHiPr     C(O)Me                                           CH(Me)CH.sub.2                                                                          C(O)imidazole                                                                          CH(Me)CH.sub.2                                                                          C(O)Me                                           CHCN      C(O)imidazole                                                                          CHCN      C(O)Me                                           CHCH.sub.2 OH                                                                           C(O)imidazole                                                                          CHCH.sub.2 OH                                                                           C(O)Me                                           CH(CH.sub.2 OH)CH.sub.2                                                                 C(O)imidazole                                                                          CH(CH.sub.2 OH)CH.sub.2                                                                 C(O)Me                                           2-Q-7; G = S; R.sup.6 = H                                                                        2-Q-7; G = S; R.sup.6 = 6-Cl                               A         R.sup.5  A         R.sup.5                                          CH.sub.2  CH.sub.2 CN                                                                            CH.sub.2  H                                                CH.sub.2 CH.sub.2                                                                       CH.sub.2 CN                                                                            CH.sub.2 CH.sub.2                                                                       H                                                CHMe      CH.sub.2 CN                                                                            CHMe      H                                                CHEt      CH.sub.2 CN                                                                            CHEt      H                                                CHiPr     CH.sub.2 CN                                                                            CHiPr     H                                                CH(Me)CH.sub.2                                                                          CH.sub.2 CN                                                                            CH(Me)CH.sub.2                                                                          H                                                CHCN      CH.sub.2 CN                                                                            CHCN      H                                                CHCH.sub.2 OH                                                                           CH.sub.2 CN                                                                            CHCH.sub.2 OH                                                                           H                                                2-Q-7; G = S; R.sup.6 = H                                                                        2-Q-7; G = S; R.sup.6 = 6-Cl                               A         R.sup.5  A         R.sup.5                                          CH(CH.sub.2 OH)CH.sub.2                                                                 CH.sub.2 CN                                                                            CH(CH.sub.2 OH)CH.sub.2                                                                 H                                                CH.sub.2  CH.sub.2 OEt                                                                           CH.sub.2  Me                                               CH.sub.2 CH.sub.2                                                                       CH.sub.2 OEt                                                                           CH.sub.2 CH.sub.2                                                                       Me                                               CHMe      CH.sub.2 OEt                                                                           CHMe      Me                                               CHEt      CH.sub.2 OEt                                                                           CHEt      Me                                               CHiPr     CH.sub.2 OEt                                                                           CHiPr     Me                                               CH(Me)CH.sub.2                                                                          CH.sub.2 OEt                                                                           CH(Me)CH.sub.2                                                                          Me                                               CHCN      CH.sub.2 OEt                                                                           CHCN      Me                                               CHCH.sub.2 OH                                                                           CH.sub.2 OEt                                                                           CHCH.sub.2 OH                                                                           Me                                               CH(CH.sub.2 OH)CH.sub.2                                                                 CH.sub.2 OEt                                                                           CH(CH.sub.2 OH)CH.sub.2                                                                 Me                                               CH.sub.2  SNBu.sub.2                                                                             CH.sub.2  C(O)imidazole                                    CH.sub.2 CH.sub.2                                                                       SNBu.sub.2                                                                             CH.sub.2 CH.sub.2                                                                       C(O)imidazole                                    CHMe      SNBu.sub.2                                                                             CHMe      C(O)imidazole                                    CHEt      SNBu.sub.2                                                                             CHEt      C(O)imidazole                                    CHiPr     SNBu.sub.2                                                                             CHiPr     C(O)imidazole                                    CH(Me)CH.sub.2                                                                          SNBu.sub.2                                                                             CH(Me)CH.sub.2                                                                          C(O)imidazole                                    CHCN      SNBu.sub.2                                                                             CHCN      C(O)imidazole                                    CHCH.sub.2 OH                                                                           SNBu.sub.2                                                                             CHCH.sub.2 OH                                                                           C(O)imidazole                                    CH(CH.sub.2 OH)CH.sub.2                                                                 SNBu.sub.2                                                                             CH(CH.sub.2 OH)CH.sub.2                                                                 C(O)imidazole                                    2-Q-7; G = S; R.sup.6 = 6-Cl                                                                     2-Q-7; G = S; R.sup.6 = 7-Cl                               A         R.sup.5  A         R.sup.5                                          CH.sub.2  SN(Me)CO.sub.2 Bu                                                                      CHCH.sub.2 OH                                                                           Me                                               CH.sub.2 CH.sub.2                                                                       SN(Me)CO.sub.2 Bu                                                                      CH(CH.sub.2 OH)CH.sub.2                                                                 Me                                               CHMe      SN(Me)CO.sub.2 Bu                                                                      CH.sub.2  C(O)imidazole                                    CHEt      SN(Me)CO.sub.2 Bu                                                                      CH.sub.2 CH.sub.2                                                                       C(O)imidazole                                    CHiPr     SN(Me)CO.sub.2 Bu                                                                      CHMe      C(O)imidazole                                    CH(Me)CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                                                                      CHEt      C(O)imidazole                                    CHCN      SN(Me)CO.sub.2 Bu                                                                      CHiPr     C(O)imidazole                                    CHCH.sub.2 OH                                                                           SN(Me)CO.sub.2 Bu                                                                      CH(Me)CH.sub.2                                                                          C(O)imidazole                                    CH(CH.sub.2 OH)CH.sub.2                                                                 SN(Me)CO.sub.2 Bu                                                                      CHCN      C(O)imidazole                                    2-Q-7; G = S; R.sup.6 = 7-Cl                                                                     2-Q-7; G = S; R.sup.6 = 7-Cl                               A         R.sup.5  A         R.sup.5                                          CH.sub.2  H        CHCH.sub.2 OH                                                                           C(O)imidazole                                    CH.sub.2 CH.sub.2                                                                       H        CH(CH.sub.2 OH)CH.sub.2                                                                 C(O)imidazole                                    CHMe      H        CH.sub.2  SN(Me)CO.sub.2 Bu                                CHEt      H        CH.sub.2 CH.sub.2                                                                       SN(Me)CO.sub.2 Bu                                CHiPr     H        CHMe      SN(Me)CO.sub.2 Bu                                CH(Me)CH.sub.2                                                                          H        CHEt      SN(Me)CO.sub.2 Bu                                CHCN      H        CHiPr     SN(Me)CO.sub.2 Bu                                CHCH.sub.2 OH                                                                           H        CH(Me)CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                                CH(CH.sub.2 OH)CH.sub.2                                                                 H        CHCN      SN(Me)CO.sub.2 Bu                                CH.sub.2  Me       CHCH.sub.2 OH                                                                           SN(Me)CO.sub.2 Bu                                CH.sub.2 CH.sub.2                                                                       Me       CH(CH.sub.2 OH)CH.sub.2                                                                 SN(Me)CO.sub.2 Bu                                CHMe      Me                                                                  CHEt      Me       3-Q-7; G = S; R.sup.6 = H                                  CHiPr     Me       A         R.sup.5                                          CH(Me)CH.sub.2                                                                          Me       CH.sub.2  H                                                CHCN      Me       CH.sub.2 CH.sub.2                                                                       H                                                                   CHMe      H                                                3-Q-7; G = S; R.sup.6 = H                                                                        CHEt      H                                                A         R.sup.5  CHiPr     H                                                CH(Me)CH.sub.2                                                                          H        CHCH.sub.2 OH                                                                           SN(Me)CO.sub.2 Bu                                CHCN      H        CH(CH.sub.2 OH)CH.sub.2                                                                 SN(Me)CO.sub.2 Bu                                CHCH.sub.2 OH                                                                           H                                                                   CH(CH.sub.2 OH)CH.sub.2                                                                 H                                                                   CH.sub.2  Me                                                                  CH.sub.2 CH.sub.2                                                                       Me                                                                  CHMe      Me                                                                  3-Q-7; G = S; R.sup.6 = H                                                                        3-Q-7; G = S; R.sup.6 = 6-Cl                               A         R.sup. 5 A         R.sup.5                                          CHEt      Me       CH.sub.2  H                                                CHiPr     Me       CH.sub.2 CH.sub.2                                                                       H                                                CH(Me)CH.sub.2                                                                          Me       CHMe      H                                                CHCN      Me       CHEt      H                                                CHCH.sub.2 OH                                                                           Me       CHiPr     H                                                CH(CH.sub.2 OH)CH.sub.2                                                                 Me       CH(Me)CH.sub.2                                                                          H                                                CH.sub.2  C(O)imidazole                                                                          CHCN      H                                                CH.sub.2 CH.sub.2                                                                       C(O)imidazole                                                                          CHCH.sub.2 OH                                                                           H                                                CHMe      C(O)imidazole                                                                          CH(CH.sub.2 OH)CH.sub.2                                                                 H                                                CHEt      C(O)imidazole                                                                          CH.sub.2  Me                                               CHiPr     C(O)imidazole                                                                          CH.sub.2 CH.sub.2                                                                       Me                                               CH(Me)CH.sub.2                                                                          C(O)imidazole                                                                          CHMe      Me                                               CHCN      C(O)imidazole                                                                          CHEt      Me                                               CHCH.sub.2 OH                                                                           C(O)imidazole                                                                          CHiPr     Me                                               CH(CH.sub.2 OH)CH.sub.2                                                                 C(O)imidazole                                                                          CH(Me)CH.sub.2                                                                          Me                                               CH.sub.2  SN(Me)CO.sub.2 Bu                                                                      CHCN      Me                                               CH.sub.2 CH.sub.2                                                                       SN(Me)CO.sub.2 Bu                                                                      CHCH.sub.2 OH                                                                           Me                                               CHMe      SN(Me)CO.sub.2 Bu                                                                      CH(CH.sub.2 OH)CH.sub.2                                                                 Me                                               CHEt      SN(Me)CO.sub.2 Bu                                                                      CH.sub.2  C(O)imidazole                                    CHiPr     SN(Me)CO.sub.2 Bu                                                                      CH.sub.2 CH.sub.2                                                                       C(O)imidazole                                    CH(Me)CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                                                                      CHMe      C(O)imidazole                                    CHCN      SN(Me)CO.sub.2 Bu                                                                      CHEt      C(O)imidazole                                                       CHiPr     C(O)imidazole                                    3-Q-7; G = S; R.sup.6 = 6-Cl                                                                      3-Q-7; G = S; R.sup.6 = 7-Cl                              A         R.sup.5  A         R.sup. 5                                         CH(Me)CH.sub.2                                                                          C(O)imidazole                                                                          CHEt      Me                                               CHCN      C(O)imidazole                                                                          CHiPr     Me                                               CHCH.sub.2 OH                                                                           C(O)imidazole                                                                          CH(Me)CH.sub.2                                                                          Me                                               CH(CH.sub.2 OH)CH.sub.2                                                                 C(O)imidazole                                                                          CHCN      Me                                               CH.sub.2  SN(Me)CO.sub.2 Bu                                                                      CHCH.sub.2 OH                                                                           Me                                               CH.sub.2 CH.sub.2                                                                       SN(Me)CO.sub.2 Bu                                                                      CH(CH.sub.2 OH)CH.sub.2                                                                 Me                                               CHMe      SN(Me)CO.sub.2 Bu                                                                      CH.sub.2  C(O)imidazole                                    CHEt      SN(Me)CO.sub.2 Bu                                                                      CH.sub.2 CH.sub.2                                                                       C(O)imidazole                                    CHiPr     SN(Me)CO.sub.2 Bu                                                                      CHMe      C(O)imidazole                                    CH(Me)CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                                                                      CHEt      C(O)imidazole                                    CHCN      SN(Me)CO.sub.2 Bu                                                                      CHiPr     C(O)imidazole                                    CHCH.sub.2 OH                                                                           SN(Me)CO.sub.2 Bu                                                                      CH(Me)CH.sub.2                                                                          C(O)imidazole                                    CH(CH.sub.2 OH)CH.sub.2                                                                 SN(Me)CO.sub.2 Bu                                                                      CHCN      C(O)imidazole                                                       CHCH.sub.2 OH                                                                           C(O)imidazole                                    3-Q-7; G = S; R.sup.6 = 7-Cl                                                                     CH(CH.sub.2 OH)CH.sub.2                                                                 C(O)imidazole                                    A         R.sup.5  CH.sub.2  SN(Me)CO.sub.2 Bu                                CH.sub.2  H        CH.sub.2 CH.sub.2                                                                       SN(Me)CO.sub.2 Bu                                CH.sub.2 CH.sub.2                                                                       H        CHMe      SN(Me)CO.sub.2 Bu                                CHMe      H        CHEt      SN(Me)CO.sub.2 Bu                                CHEt      H        CHiPr     SN(Me)CO.sub.2 Bu                                CHiPr     H        CH(Me)CH.sub.2                                                                          SN(Me)CO.sub.2 Bu                                CH(Me)CH.sub.2                                                                          H        CHCN      SN(Me)CO.sub.2 Bu                                CHCN      H        CHCH.sub.2 OH                                                                           SN(Me)CO.sub.2 Bu                                CHCH.sub.2 OH                                                                           H        CH(CH.sub.2 OH)CH.sub. 2                                                                SN(Me)CO.sub.2 Bu                                CH(CH.sub.2 OH)CH.sub.2                                                                 H                                                                   CH.sub.2  Me                                                                  CH.sub.2 CH.sub.2                                                                       Me                                                                  CHMe      Me                                                                  __________________________________________________________________________

                  TABLE 8                                                         ______________________________________                                         ##STR26##                                                                    A           R.sup.5                                                                              A             R.sup.5                                      ______________________________________                                        6-Q-8; G = O;                                                                 R.sup.6 = H; R.sup.7 = H                                                                     6-Q-8; G = O; R.sup.6 = H; R.sup.7 = H                         CH.sub.2    H      CH.sub.2      C(O)imidazole                                CH.sub.2 CH.sub.2                                                                         H      CH.sub.2 CH.sub.2                                                                           C(O)imidazole                                CHMe        H      CHMe          C(O)imidazole                                CHEt        H      CHEt          C(O)imidazole                                CHiPr       H      CHiPr         C(O)imidazole                                CH(Me)CH.sub.2                                                                            H      CH(Me)CH.sub.2                                                                              C(O)imidazole                                CHCN        H      CHCN          C(O)imidazole                                CHCH.sub.2 OH                                                                             H      CHCH.sub.2 OH C(O)imidazole                                CH(CH.sub.2 OH)CH.sub.2                                                                   H      CH(CH.sub.2 OH)CH.sub.2                                                                     C(O)imidazole                                CH.sub.2    Me     CH.sub.2      SN(Me)CO.sub.2 Bu                            CH.sub.2 CH.sub.2                                                                         Me     CH.sub.2 CH.sub.2                                                                           SN(Me)CO.sub.2 Bu                            CHMe        Me     CHMe          SN(Me)CO.sub.2 Bu                            CHEt        Me     CHEt          SN(Me)CO.sub.2 Bu                            CHiPr       Me     CHiPr         SN(Me)CO.sub.2 Bu                            CH(Me)CH.sub.2                                                                            Me     CH(Me)CH.sub.2                                                                              SN(Me)CO.sub.2 Bu                            CHCN        Me     CHCN          SN(Me)CO.sub.2 Bu                            CHCH.sub.2 OH                                                                             Me     CHCH.sub.2 OH SN(Me)CO.sub.2 Bu                            CH(CH.sub.2 OH)CH.sub.2                                                                   Me     CH(CH.sub.2 OH)CH.sub.2                                                                     SN(Me)CO.sub.2 Bu                            6-Q-8; G = O;                                                                 R.sup.6 = H; R.sup.7 = Cl                                                                    6-Q-8; G = O; R.sup.6 = H; R.sup.7 = Cl                        CH.sub.2    H      CH.sub.2      C(O)imidazole                                CH.sub.2 CH.sub.2                                                                         H      CH.sub.2 CH.sub.2                                                                           C(O)imidazole                                CHMe        H      CHMe          C(O)imidazole                                CHEt        H      CHEt          C(O)imidazole                                CHiPr       H      CHiPr         C(O)imidazole                                CH(Me)CH.sub.2                                                                            H      CH(Me)CH.sub.2                                                                              C(O)imidazole                                CHCN        H      CHCN          C(O)imidazole                                CHCH.sub.2 OH                                                                             H      CHCH.sub.2 OH C(O)imidazole                                CH(CH.sub.2 OH)CH.sub.2                                                                   H      CH(CH.sub.2 OH)CH.sub.2                                                                     C(O)imidazole                                CH.sub.2    Me     CH.sub.2      SN(Me)CO.sub.2 Bu                            CH.sub.2 CH.sub.2                                                                         Me     CH.sub.2 CH.sub.2                                                                           SN(Me)CO.sub.2 Bu                            CHMe        Me     CHMe          SN(Me)CO.sub.2 Bu                            CHEt        Me     CHEt          SN(Me)CO.sub.2 Bu                            CHiPr       Me     CHiPr         SN(Me)CO.sub.2 Bu                            CH(Me)CH.sub. 2                                                                           Me     CH(Me)CH.sub.2                                                                              SN(Me)CO.sub.2 Bu                            CHCN        Me     CHCN          SN(Me)CO.sub.2 Bu                            CHCH.sub.2 OH                                                                             Me     CHCH.sub.2 OH SN(Me)CO.sub.2 Bu                            CH(CH.sub.2 OH)CH.sub.2                                                                   Me     CH(CH.sub.2 OH)CH.sub.2                                                                     SN(Me)CO.sub.2 Bu                            6-Q-8; G = O;                                                                 R.sup.6 = Cl; R.sup.7 = H                                                                    6-Q-8; G = O; R.sup.6 = Cl; R.sup.7 = H                        CH.sub.2    H      CH.sub.2      C(O)imidazole                                CH.sub.2 CH.sub.2                                                                         H      CH.sub.2 CH.sub.2                                                                           C(O)imidazole                                CHMe        H      CHMe          C(O)imidazole                                CHEt        H      CHEt          C(O)imidazole                                CHiPr       H      CHiPr         C(O)imidazole                                6-Q-8; G = O;                                                                 R.sup.6 = Cl; R.sup.7 = H                                                                    6-Q-8; G = O; R.sup.6 = Cl; R.sup.7 = H                        CH(Me)CH.sub.2                                                                            H      CH(Me)CH.sub.2                                                                              C(O)imidazole                                CHCN        H      CHCN          C(O)imidazole                                CHCH.sub.2 OH                                                                             H      CHCH.sub.2 OH C(O)imidazole                                CH(CH.sub.2 OH)CH.sub.2                                                                   H      CH(CH.sub.2 OH)CH.sub.2                                                                     C(O)imidazole                                CH.sub.2    Me     CH.sub.2      SN(Me)CO.sub.2 Bu                            CH.sub.2 CH.sub.2                                                                         Me     CH.sub.2 CH.sub.2                                                                           SN(Me)CO.sub.2 Bu                            CHMe        Me     CHMe          SN(Me)CO.sub.2 Bu                            CHEt        Me     CHEt          SN(Me)CO.sub.2 Bu                            CHiPr       Me     CHiPr         SN(Me)CO.sub.2 Bu                            CH(Me)CH.sub.2                                                                            Me     CH(Me)CH.sub.2                                                                              SM(Me)CO.sub.2 Bu                            CHCN        Me     CHCN          SN(Me)CO.sub.2 Bu                            CHCH.sub.2 OH                                                                             Me     CHCH.sub.2 OH SN(Me)CO.sub.2 Bu                            CH(CH.sub.2 OH)CH.sub.2                                                                   Me     CH(CH.sub.2 OH)CH.sub.2                                                                     SN(Me)CO.sub.2 Bu                            7-Q-8; G = O;                                                                 R.sup.6 = H; R.sup.7 = H                                                                     7-Q-8; G = O; R.sup.6 = H; R.sup.7 = H                         CH.sub.2    H      CH.sub.2      C(O)imidazole                                CH.sub.2 CH.sub.2                                                                         H      CH.sub.2 CH.sub.2                                                                           C(O)imidazole                                CHMe        H      CHMe          C(O)imidazole                                CHEt        H      CHEt          C(O)imidazole                                CHiPr       H      CHiPr         C(O)imidazole                                CH(Me)CH.sub.2                                                                            H      CH(Me)CH.sub.2                                                                              C(O)imidazole                                CHCN        H      CHCN          C(O)imidazole                                CHCH.sub.2 OH                                                                             H      CHCH.sub.2 OH C(O)imidazole                                7-Q-8; G = O;                                                                 R.sup.6 = H; R.sup.7 = H                                                                     7-Q-8; G = O; R.sup.6 = H; R.sup.7 = H                         CH(CH.sub.2 OH)CH.sub.2                                                                   H      CH(CH.sub.2 OH)CH.sub.2                                                                     C(O)imidazole                                CH.sub.2    Me     CH.sub.2      SN(Me)CO.sub.2 Bu                            CH.sub.2 CH.sub.2                                                                         Me     CH.sub.2 CH.sub.2                                                                           SN(Me)CO.sub.2 Bu                            CHMe        Me     CHMe          SN(Me)CO.sub.2 Bu                            CHEt        Me     CHEt          SN(Me)CO.sub.2 Bu                            CHiPr       Me     CHiPr         SN(Me)CO.sub.2 Bu                            CH(Me)CH.sub.2                                                                            Me     CH(Me)CH.sub.2                                                                              SN(Me)CO.sub.2 Bu                            CHCN        Me     CHCN          SN(Me)CO.sub.2 Bu                            CHCH.sub.2 OH                                                                             Me     CHCH.sub.2 OH SN(Me)CO.sub.2 Bu                            CH(CH.sub.2 OH)CH.sub.2                                                                   Me     CH(CH.sub.2 OH)CH.sub.2                                                                     SN(Me)CO.sub.2 Bu                            7-Q-8; G = O;                                                                 R.sup.6 = H; R.sup.7 = Cl                                                                    7-Q-8; G = O; R.sup.6 = H; R.sup.7 = Cl                        CH.sub.2    H      CH.sub.2      C(O)imidazole                                CH.sub.2 CH.sub.2                                                                         H      CH.sub.2 CH.sub.2                                                                           C(O)imidazole                                CHMe        H      CHMe          C(O)imidazole                                CHEt        H      CHEt          C(O)imidazole                                CHiPr       H      CHiPr         C(O)imidazole                                CH(Me)CH.sub.2                                                                            H      CH(Me)CH.sub.2                                                                              C(O)imidazole                                CHCN        H      CHCN          C(O)imidazole                                CHCH.sub.2 OH                                                                             H      CHCH.sub.2 OH C(O)imidazole                                CH(CH.sub.2 OH)CH.sub.2                                                                   H      CH(CH.sub.2 OH)CH.sub.2                                                                     C(O)imidazole                                CH.sub.2    Me     CH.sub.2      SN(Me)CO.sub.2 Bu                            CH.sub.2 CH.sub.2                                                                         Me     CH.sub.2 CH.sub.2                                                                           SN(Me)CO.sub.2 Bu                            7-Q-8; G = O;                                                                 R.sup.6 =  H; R.sup.7 = Cl                                                                   7-Q-8; G = O; R.sup.6 = H; R.sup.7 = Cl                        CHMe        Me     CHMe          SN(Me)CO.sub.2 Bu                            CHEt        Me     CHEt          SN(Me)CO.sub.2 Bu                            CHiPr       Me     CHiPr         SN(Me)CO.sub.2 Bu                            CH(Me)CH.sub.2                                                                            Me     CH(Me)CH.sub.2                                                                              SN(Me)CO.sub.2 Bu                            CHCN        Me     CHCN          SN(Me)CO.sub.2 Bu                            CHCH.sub.2 OH                                                                             Me     CHCH.sub.2 OH SN(Me)CO.sub.2 Bu                            CH(CH.sub.2 OH)CH.sub.2                                                                   Me     CH(CH.sub.2 OH)CH.sub.2                                                                     SN(Me)CO.sub.2 Bu                            7-Q-8; G = O;                                                                 R.sup.6 = Cl; R.sup.7 = H                                                                    7-Q-8; G = O; R.sup.6 = Cl; R.sup.7 = H                        CH.sub.2    H      CH.sub.2      C(O)imidazole                                CH.sub.2 CH.sub.2                                                                         H      CH.sub.2 CH.sub.2                                                                           C(O)imidazole                                CHMe        H      CHMe          C(O)imidazole                                CHEt        H      CHEt          C(O)imidazole                                CHiPr       H      CHiPr         C(O)imidazole                                CH(Me)CH.sub.2                                                                            H      CH(Me)CH.sub.2                                                                              C(O)imidazole                                CHCN        H      CHCN          C(O)imidazole                                CHCH.sub.2 OH                                                                             H      CHCH.sub.2 OH C(O)imidazole                                CH(CH.sub.2 OH)CH.sub.2                                                                   H      CH(CH.sub.2 OH)CH.sub.2                                                                     C(O)imidazole                                CH.sub.2    Me     CH.sub.2      SN(Me)CO.sub.2 Bu                            CH.sub.2 CH.sub.2                                                                         Me     CH.sub.2 CH.sub.2                                                                           SN(Me)CO.sub. 2 Bu                           CHMe        Me     CHMe          SN(Me)CO.sub.2 Bu                            CHEt        Me     CHEt          SN(Me)CO.sub.2 Bu                            CHiPr       Me     CHiPr         SN(Me)CO.sub.2 Bu                            CH(Me)CH.sub.2                                                                            Me     CH(Me)CH.sub.2                                                                              SN(Me)CO.sub.2 Bu                            CHCN        Me     CHCN          SN(Me)CO.sub.2 Bu                            CHCH.sub.2 OH                                                                             Me     CHCH.sub.2 OH SN(Me)CO.sub.2 Bu                            CH(CH.sub.2 OH)CH.sub.2                                                                   Me     CH(CH.sub.2 OH)CH.sub.2                                                                     SN(Me)CO.sub.2 Bu                            6-Q-8; G = S;                                                                 R.sup.6 = H; R.sup.7 = H                                                                     6-Q-8; G = S; R.sup.6 = H; R.sup.7 = H                         CH.sub.2    H      CH.sub.2      C(O)imidazole                                CH.sub.2 CH.sub.2                                                                         H      CH.sub.2 CH.sub.2                                                                           C(O)imidazole                                CHMe        H      CHMe          C(O)imidazole                                CHEt        H      CHEt          C(O)imidazole                                CHiPr       H      CHiPr         C(O)imidazole                                CH(Me)CH.sub.2                                                                            H      CH(Me)CH.sub.2                                                                              C(O)imidazole                                CHCN        H      CHCN          C(O)imidazole                                CHCH.sub.2 OH                                                                             H      CHCH.sub.2 OH C(O)imidazole                                CH(CH.sub.2 OH)CH.sub.2                                                                   H      CH(CH.sub.2 OH)CH.sub.2                                                                     C(O)imidazole                                CH.sub.2    Me     CH.sub.2      SN(Me)CO.sub.2 Bu                            CH.sub.2 CH.sub.2                                                                         Me     CH.sub.2 CH.sub.2                                                                           SN(Me)CO.sub.2 Bu                            CHMe        Me     CHMe          SN(Me)CO.sub.2 Bu                            CHEt        Me     CHEt          SN(Me)CO.sub.2 Bu                            CHiPr       Me     CHiPr         SN(Me)CO.sub.2 Bu                            CH(Me)CH.sub.2                                                                            Me     CH(Me)CH.sub.2                                                                              SN(Me)CO.sub.2 Bu                            CHCN        Me     CHCN          SN(Me)CO.sub.2 Bu                            CHCH.sub.2 OH                                                                             Me     CHCH.sub.2 OH SN(Me)CO.sub.2 Bu                            CH(CH.sub.2 OH)CH.sub.2                                                                   Me     CH(CH.sub.2 OH)CH.sub.2                                                                     SN(Me)CO.sub.2 Bu                            6-Q-8; G = S;                                                                 R.sup.6 = H; R.sup.7 = Cl                                                                    6-Q-8; G = S; R.sup.6 = H; R.sup.7 = Cl                        CH.sub.2    H      CH.sub.2      C(O)imidazole                                CH.sub.2 CH.sub.2                                                                         H      CH.sub.2 CH.sub.2                                                                           C(O)imidazole                                CHMe        H      CHMe          C(O)imidazole                                CHEt        H      CHEt          C(O)imidazole                                CHiPr       H      CHiPr         C(O)imidazole                                CH(Me)CH.sub.2                                                                            H      CH(Me)CH.sub.2                                                                              C(O)imidazole                                CHCN        H      CHCN          C(O)imidazole                                6-Q-8; G = S;                                                                 R.sup.6 = H; R.sup.7 = Cl                                                                    6-Q-8; G = S; R.sup.6 = H; R.sup.7 = Cl                        CHCH.sub.2 OH                                                                             H      CHCH.sub.2 OH C(O)imidazole                                CH(CH.sub.2 OH)CH.sub.2                                                                   H      CH(CH.sub.2 OH)CH.sub.2                                                                     C(O)imidazole                                CH.sub.2    Me     CH.sub.2      SN(Me)CO.sub.2 Bu                            CH.sub.2 CH.sub.2                                                                         Me     CH.sub.2 CH.sub.2                                                                           SN(Me)CO.sub.2 Bu                            CHMe        Me     CHMe          SN(Me)CO.sub.2 Bu                            CHEt        Me     CHEt          SN(Me)CO.sub.2 Bu                            CHiPr       Me     CHiPr         SN(Me)CO.sub.2 Bu                            CH(Me)CH.sub.2                                                                            Me     CH(Me)CH.sub.2                                                                              SN(Me)CO.sub.2 Bu                            CHCN        Me     CHCN          SN(Me)CO.sub.2 Bu                            CHCH.sub.2 OH                                                                             Me     CHCH.sub.2 OH SN(Me)CO.sub.2 Bu                            CH(CH.sub.2 OH)CH.sub.2                                                                   Me     CH(CH.sub.2 OH)CH.sub.2                                                                     SN(Me)CO.sub.2 Bu                            6-Q-8; G = S;                                                                 R.sup.6 = Cl; R.sup.7 = H                                                                    6-Q-8; G = S; R.sup.6 = Cl; R.sup.7 = H                        CH.sub.2    H      CH.sub.2      C(O)imidazole                                CH.sub.2 CH.sub.2                                                                         H      CH.sub.2 CH.sub.2                                                                           C(O)imidazole                                CHMe        H      CHMe          C(O)imidazole                                CHEt        H      CHEt          C(O)imidazole                                CHiPr       H      CHiPr         C(O)imidazole                                CH(Me)CH.sub.2                                                                            H      CH(Me)CH.sub.2                                                                              C(O)imidazole                                CHCN        H      CHCN          C(O)imidazole                                CHCH.sub.2 OH                                                                             H      CHCH.sub.2 OH C(O)imidazole                                CH(CH.sub.2 OH)CH.sub.2                                                                   H      CH(CH.sub.2 OH)CH.sub.2                                                                     C(O)imidazole                                CH.sub.2    Me     CH.sub.2      SN(Me)CO.sub.2 Bu                            CH.sub.2 CH.sub.2                                                                         Me     CH.sub.2 CH.sub.2                                                                           SN(Me)CO.sub.2 Bu                            CHMe        Me     CHMe          SN(Me)CO.sub.2 Bu                            6-Q-8; G = S;                                                                 R.sup.6 = Cl; R.sup.7 = H                                                                    6-Q-8; G = S; R.sup.6  = Cl; R.sup.7 = H                       CHEt        Me     CHEt          SN(Me)CO.sub.2 Bu                            CHiPr       Me     CHiPr         SN(Me)CO.sub.2 Bu                            CH(Me)CH.sub.2                                                                            Me     CH(Me)CH.sub.2                                                                              SN(Me)CO.sub.2 Bu                            CHCN        Me     CHCN          SN(Me)CO.sub.2 Bu                            CHCH.sub.2 OH                                                                             Me     CHCH.sub.2 OH SN(Me)CO.sub.2 Bu                            CH(CH.sub.2 OH)CH.sub.2                                                                   Me     CH(CH.sub.2 OH)CH.sub.2                                                                     SN(Me)CO.sub.2 Bu                            7-Q-8; G = S;                                                                 R.sup.6 = H; R.sup.7 = H                                                                     7-Q-8; G = S; R.sup.6 = H; R.sup.7 = H                         CH.sub.2    H      CH.sub.2      C(O)imidazole                                CH.sub.2 CH.sub.2                                                                         H      CH.sub.2 CH.sub.2                                                                           C(O)imidazole                                CHMe        H      CHMe          C(O)imidazole                                CHEt        H      CHEt          C(O)imidazole                                CHiPr       H      CHiPr         C(O)imidazole                                CH(Me)CH.sub.2                                                                            H      CH(Me)CH.sub.2                                                                              C(O)imidazole                                CHCN        H      CHCN          C(O)imidazole                                CHCH.sub.2 OH                                                                             H      CHCH.sub.2 OH C(O)imidazole                                CH(CH.sub.2 OH)CH.sub.2                                                                   H      CH(CH.sub.2 OH)CH.sub.2                                                                     C(O)imidazole                                CH.sub.2    Me     CH.sub.2      SN(Me)CO.sub.2 Bu                            CH.sub.2 CH.sub.2                                                                         Me     CH.sub.2 CH.sub.2                                                                           SN(Me)CO.sub.2 Bu                            CHMe        Me     CHMe          SN(Me)CO.sub.2 Bu                            CHEt        Me     CHEt          SN(Me)CO.sub.2 Bu                            CHiPr       Me     CHiPr         SN(Me)CO.sub.2 Bu                            CH(Me)CH.sub.2                                                                            Me     CH(Me)CH.sub.2                                                                              SN(Me)CO.sub.2 Bu                            CHCN        Me     CHCN          SN(Me)CO.sub.2 Bu                            CHCH.sub.2 OH                                                                             Me     CHCH.sub.2 OH SN(Me)CO.sub.2 Bu                            CH(CH.sub.2 OH)CH.sub.2                                                                   Me     CH(CH.sub.2 OH)CH.sub.2                                                                     SN(Me)CO.sub.2 Bu                            7-Q-8; G = S;                                                                 R.sup.6 = H; R.sup.7 = Cl                                                                    7-Q-8; G = S; R.sup.6 = H; R.sup.7 = Cl                        CH.sub.2    H      CH.sub.2      C(O)imidazole                                CH.sub.2 CH.sub.2                                                                         H      CH.sub.2 CH.sub.2                                                                           C(O)imidazole                                CHMe        H      CHMe          C(O)imidazole                                CHEt        H      CHEt          C(O)imidazole                                CHiPr       H      CHiPr         C(O)imidazole                                CH(Me)CH.sub.2                                                                            H      CH(Me)CH.sub.2                                                                              C(O)imidazole                                CHCN        H      CHCN          C(O)imidazole                                CHCH.sub.2 OH                                                                             H      CHCH.sub.2 OH C(O)imidazole                                CH(CH.sub.2 OH)CH.sub.2                                                                   H      CH(CH.sub.2 OH)CH.sub.2                                                                     C(O)imidazole                                CH.sub.2    Me     CH.sub.2      SN(Me)CO.sub.2 Bu                            CH.sub.2 CH.sub.2                                                                         Me     CH.sub.2 CH.sub.2                                                                           SN(Me)CO.sub.2 Bu                            CHMe        Me     CHMe          SN(Me)CO.sub.2 Bu                            CHEt        Me     CHEt          SN(Me)CO.sub.2 Bu                            CHiPr       Me     CHiPr         SN(Me)CO.sub.2 Bu                            CH(Me)CH.sub.2                                                                            Me     CH(Me)CH.sub.2                                                                              SN(Me)CO.sub.2 Bu                            CHCN        Me     CHCN          SN(Me)CO.sub.2 Bu                            CHCH.sub.2 OH                                                                             Me     CHCH.sub.2 OH SN(Me)CO.sub.2 Bu                            CH(CH.sub.2 OH)CH.sub.2                                                                   Me     CH(CH.sub.2 OH)CH.sub.2                                                                     SN(Me)CO.sub.2 Bu                            7-Q-8; G = S;                                                                 R.sup.6 = Cl; R.sup.7 = H                                                                    7-Q-8; G = S; R.sup.6 = Cl; R.sup.7 = H                        CH.sub.2    H      CH.sub.2      C(O)imidazole                                CH.sub.2 CH.sub.2                                                                         H      CH.sub.2 CH.sub.2                                                                           C(O)imidazole                                CHMe        H      CHMe          C(O)imidazole                                CHEt        H      CHEt          C(O)imidazole                                CHiPr       H      CHiPr         C(O)imidazole                                CH(Me)CH.sub.2                                                                            H      CH(Me)CH.sub.2                                                                              C(O)imidazole                                CHCN        H      CHCN          C(O)imidazole                                CHCH.sub.2 OH                                                                             H      CHCH.sub.2 OH C(O)imidazole                                7-Q-8; G = S;                                                                 R.sup.6 = Cl; R.sup.7 = H                                                                    7-Q-8; G = S; R.sup.6 = Cl; R.sup.7 = H                        CH(CH.sub.2 OH)CH.sub.2                                                                   H      CH(CH.sub.2 OH)CH.sub.2                                                                     C(O)imidazole                                CH.sub.2    Me     CH.sub.2      SN(Me)CO.sub.2 Bu                            CH.sub.2 CH.sub.2                                                                         Me     CH.sub.2 CH.sub.2                                                                           SN(Me)CO.sub.2 Bu                            CHMe        Me     CHMe          SN(Me)CO.sub.2 Bu                            CHEt        Me     CHEt          SN(Me)CO.sub.2 Bu                            CHiPr       Me     CHiPr         SN(Me)CO.sub.2 Bu                            CH(Me)CH.sub.2                                                                            Me     CH(Me)CH.sub.2                                                                              SN(Me)CO.sub.2 Bu                            CHCN        Me     CHCN          SN(Me)CO.sub.2 Bu                            CHCH.sub.2 OH                                                                             Me     CHCH.sub.2 OH SN(Me)CO.sub.2 Bu                            CH(CH.sub.2 OH)CH.sub.2                                                                   Me     CH(CH.sub.2 OH)CH.sub.2                                                                     SN(Me)CO.sub.2 Bu                            ______________________________________                                    

                  TABLE 9                                                         ______________________________________                                         ##STR27##                                                                    A                 A                                                           ______________________________________                                        4-GeMe.sub.3 ; R.sup.5 = H; R.sup.13 = Me                                                       3-GeMe.sub.3 ; R.sup.5 = H; R.sup.13 = Me                   CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CH.sub.2 CH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2                                  CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH.sub.2 CHMe     CH.sub.2 CHMe                                               CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CH(Me)CH.sub.2 CH.sub.2                                                                         CH(Me)CH.sub.2 CH.sub.2                                     CH.sub.2 CH(Me)CH.sub.2                                                                         CH.sub.2 CH(Me)CH.sub.2                                     CMe.sub.2         CMe.sub.2                                                   CHCO.sub.2 Me     CHCO.sub.2 Me                                               CHC(O)Me          CHC(O)Me                                                    CHCN              CHCN                                                        CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     4-GeMe.sub.3 ; R.sup.5 = Me; R.sup. 13 = Me                                                     3-GeMe.sub.3 ; R.sup.5 = Me; R.sup.13 = Me                  CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CH.sub.2 CH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2                                  4-GeMe.sub.3 ; R.sup.5 = Me; R.sup.13 = Me                                                      3-GeMe.sub.3 ; R.sup.5 = Me; R.sup.13 = Me                  CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH.sub.2 CHMe     CH.sub.2 CHMe                                               CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CH(Me)CH.sub.2 CH.sub.2                                                                         CH(Me)CH.sub.2 CH.sub.2                                     CH.sub.2 CH(Me)CH.sub.2                                                                         CH.sub.2 CH(Me)CH.sub.2                                     CMe.sub.2         CMe.sub.2                                                   CHCO.sub.2 Me     CHCO.sub.2 Me                                               CHC(O)Me          CHC(O)Me                                                    CHCN              CHCN                                                        CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     4-GeMe.sub.3 ; R.sup.5 = Et; R.sup.13 = Me                                                      3-GeMe.sub.3 ; R.sup.5 = Et; R.sup.13 = Me                  CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CH.sub.2 CH.sub.2 CH.sub.2                                                                      CH.sub. 2 CH.sub.2 CH.sub.2                                 CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH.sub.2 CHMe     CH.sub.2 CHMe                                               CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CH(Me)CH.sub.2 CH.sub.2                                                                         CH(Me)CH.sub.2 CH.sub.2                                     CH.sub.2 CH(Me)CH.sub.2                                                                         CH.sub.2 CH(Me)CH.sub.2                                     4-GeMe.sub.3 ; R.sup.5 = Et; R.sup.13 = Me                                                      3-GeMe.sub.3 ; R.sup.5 = Et; R.sup.13 = Me                  CMe.sub.2         CMe.sub.2                                                   CHCO.sub.2 Me     CHCO.sub.2 Me                                               CHC(O)Me          CHC(O)Me                                                    CHCN              CHCN                                                        CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     4-GeMe.sub.3 ;    3-GeMe.sub.3 ;                                              R.sup.5 = C(O)imidazole; R.sup.13 = Me                                                          R.sup.5 = C(O)imidazole; R.sup.13 = Me                      CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CH.sub.2 CH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2                                  CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH.sub.2 CHMe     CH.sub.2 CHMe                                               CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CH(Me)CH.sub.2 CH.sub.2                                                                         CH(Me)CH.sub.2 CH.sub.2                                     CH.sub.2 CH(Me)CH.sub.2                                                                         CH.sub.2 CH(Me)CH.sub.2                                     CMe.sub.2         CMe.sub.2                                                   CHCO.sub.2 Me     CHCO.sub.2 Me                                               CHC(O)Me          CHC(O)Me                                                    CHCN              CHCN                                                        CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     4-GeMe.sub.3 ;    3-GeMe.sub.3 ;                                              R.sup.5 = C(O)Me; R.sup.1 = Me                                                                  R.sup.5 = C(O)Me; R.sup.1 = Me                              CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CH.sub.2 CH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2                                  CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH.sub.2 CHMe     CH.sub.2 CHMe                                               CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CH(Me)CH.sub.2 CH.sub.2                                                                         CH(Me)CH.sub.2 CH.sub.2                                     CH.sub.2 CH(Me)CH.sub.2                                                                         CH.sub.2 CH(Me)CH.sub.2                                     CMe.sub.2         CMe.sub.2                                                   CHCO.sub.2 Me     CHCO.sub.2 Me                                               CHC(O)Me          CHC(O)Me                                                    CHCN              CHCN                                                        CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     4-GeMe.sub.3 ;    3-GeMe.sub.3 ;                                              R.sup.5 = CH.sub.2 CN; R.sup.13 = Me                                                            R.sup.5 = CH.sub.2 CN; R.sup.1 = Me                         CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CH.sub.2 CH.sub.2 CH.sub.2                                                                      CH.sub. 2 CH.sub.2 CH.sub.2                                 CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH.sub.2 CHMe     CH.sub.2 CHMe                                               CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              4-GeMe.sub.3 ;    3-GeMe.sub.3 ;                                              R.sup.5 = CH.sub.2 CN; R.sup.13 = Me                                                            R.sup.5 = CH.sub.2 CN; R.sup.13 = Me                        CH(Me)CH.sub.2 CH.sub.2                                                                         CH(Me)CH.sub.2 CH.sub.2                                     CH.sub.2 CH(Me)CH.sub.2                                                                         CH.sub.2 CH(Me)CH.sub.2                                     CMe.sub.2         CMe.sub.2                                                   CHCO.sub.2 Me     CHCO.sub.2 Me                                               CHC(O)Me          CHC(O)Me                                                    CHCN              CHCN                                                        CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     4-GeMe.sub.3 ;    3-GeMe.sub.3 ;                                              R.sup.5 = CH.sub.2 OEt; R.sup.13 = Me                                                           R.sup.5 = CH.sub.2 OEt; R.sup.13 = Me                       CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CH.sub.2 CH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2                                  CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH.sub.2 CHMe     CH.sub.2 CHMe                                               CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CH(Me)CH.sub.2 CH.sub.2                                                                         CH(Me)CH.sub.2 CH.sub.2                                     CH.sub.2 CH(Me)CH.sub.2                                                                         CH.sub.2 CH(Me)CH.sub. 2                                    CMe.sub.2         CMe.sub.2                                                   CHCO.sub.2 Me     CHCO.sub.2 Me                                               CHC(O)Me          CHC(O)Me                                                    CHCN              CHCN                                                        CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     4-GeMe.sub.3 ;    3-GeMe.sub.3 ;                                              R.sup.5 = SNBu.sub.2 ; R.sup.13 = Me                                                            R.sup.5 = SNBu.sub.2 ; R.sup.13 = Me                        CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CH.sub.2 CH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2                                  CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH.sub.2 CHMe     CH.sub.2 CHMe                                               CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CH(Me)CH.sub.2 CH.sub.2                                                                         CH(Me)CH.sub.2 CH.sub.2                                     CH.sub.2 CH(Me)CH.sub.2                                                                         CH.sub.2 CH(Me)CH.sub.2                                     CMe.sub.2         CMe.sub.2                                                   CHCO.sub.2 Me     CHCO.sub.2 Me                                               CHC(O)Me          CHC(O)Me                                                    CHCN              CHCN                                                        CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     4-GeMe.sub.3 ;    3-GeMe.sub.3 ;                                              R.sup.5 = SN(Me)CO.sub.2 Bu;                                                                    R.sup.5 = SN(Me)CO.sub.2 Bu;                                R.sup.13 = Me     R.sup.13 = Me                                               CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub. 2                                                                              CH.sub.2 CH.sub.2                                           CH.sub.2 CH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2                                  CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH.sub.2 CHMe     CH.sub.2 CHMe                                               CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              4-GeMe.sub.3 ;    3-GeMe.sub.3 ;                                              R.sup.5 = SN(Me)CO.sub.2 Bu;                                                                    R.sup.5 = SN(Me)CO.sub.2 Bu;                                R.sup.13 = Me     R.sup.13 = Me                                               CH(Me)CH.sub.2 CH.sub.2                                                                         CH(Me)CH.sub.2 CH.sub.2                                     CH.sub.2 CH(Me)CH.sub.2                                                                         CH.sub.2 CH(Me)CH.sub.2                                     CMe.sub.2         CMe.sub.2                                                   CHCO.sub.2 Me     CHCO.sub.2 Me                                               CHC(O)Me          CHC(O)Me                                                    CHCN              CHCN                                                        CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     4-GeMe.sub.2 R.sup.13 ;                                                                         4-GeMe.sub.2 R.sup.13 ;                                     R.sup.5 =  H; R.sup.13 = tBu                                                                    R.sup.5 = C(O)imidazole; R.sup.13 = tBu                     CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                                       4-GeMe.sub.2 R.sup.13 ;                                     4-GeMe.sub.2 R.sup.13  ;                                                                        R.sup.5 = SN(Me)CO.sub.2 Bu;                                R.sup.5 = Me; R.sup.13 = tBu                                                                    R.sup.13 = tBu                                              CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CHMe              CHMe                                                        CHEt              CHEt                                                                          4-GeMe.sub.2 R.sup.13 ;                                     4-GeMe.sub.2 R.sup.13 ;                                                                         R.sup.5 = SN(Me)CO.sub.2 Bu;                                R.sup.5 = Me; R.sup.13 = tBu                                                                    R.sup.13 = tBu                                              CHiPr             CHiPr                                                       CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                                       4-GeMe.sub.2 R.sup.13 ;                                                       R.sup.5 = C(O)imidazole;                                    4-GeMe.sub.2 R.sup.13 ; R.sup.5 = H; R.sup.13 = Ph                                              R.sup.13 = Ph                                               CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                                       4-GeMe.sub.2 R.sup.13 ;                                     4-GeMe.sub.2 R.sup.13 ;                                                                         R.sup.5 = SN(Me)CO.sub.2 Bu;                                R.sup.5 = Me; R.sup.13 = Ph                                                                     R.sup.13 = Ph                                               CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                                         4-GeMe.sub.2 R.sup.13 ;                                     4-GeMe.sub.2 R.sup.13 ;                                                                         R.sup.5 = SN(Me)CO.sub.2 Bu;                                R.sup.5 = Me; R.sup.13 = Ph                                                                     R.sup.13 = Ph                                               CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                                       4-GeMe.sub.2 R.sup.13 ;                                     4-GeMe.sub.2 R.sup.13 ;                                                                         R.sup.5 = C(O)imidazole;                                    R.sup.5 = H; R.sup.13 = CH.sub.2 OEt                                                            R.sup.13 = CH.sub.2 OEt                                     CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                                       4-GeMe.sub.2 R.sup.13 ;                                     4-GeMe.sub.2 R.sup.13 ;                                                                         R.sup.5 = SN(Me)CO.sub.2 Bu;                                R.sup.5 = Me; R.sup.13 = CH.sub.2 OEt                                                           R.sup.13 = CH.sub.2 OEt                                     CH.sub.2          CH.sub.2                                                    CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2                                           CHMe              CHMe                                                        CHEt              CHEt                                                        CHiPr             CHiPr                                                       CH(Me)CH.sub.2    CH(Me)CH.sub.2                                              CHCH.sub.2 OH     CHCH.sub.2 OH                                               CH(CH.sub.2 OH)CH.sub.2                                                                         CH(CH.sub.2 OH)CH.sub.2                                     ______________________________________                                    

Formulation and Use

The compounds of this invention will generally be used in formulationwith an agriculturally suitable carrier comprising a liquid or soliddiluent or an organic solvent. Useful formulations of the compounds ofFormula I can be prepared in conventional ways. They include dusts,granules, baits, pellets, solutions, suspensions, emulsions, wettablepowders, emulsifiable concentrates, dry flowables and the like. Many ofthese can be applied directly. Sprayable formulations can be extended insuitable media and used at spray volumes of from about one to severalhundred liters per hectare. High strength compositions are primarilyused as intermediates for further formulation. The formulations,broadly, contain from less than about 1% to 99% by weight of activeingredient(s) and at least one of a) about 0.1% to 20% surfactant (s)and b) about 5% to 99% solid or liquid diluent(s). More specifically,they will contain effective amounts of these ingredients in thefollowing approximate proportions:

    ______________________________________                                                    Percent by Weight                                                             Active                                                                        Ingredient                                                                            Diluent(s)                                                                              Surfactant(s)                                   ______________________________________                                        Wettable Powders                                                                            25-90      0-74     1-10                                        Oil Suspensions,  5-50                                                                      40-95     0-15                                                  Emulsions, Solutions,                                                         (including Emulsifiable                                                       Concentrates)                                                                 Dusts          1-25     70-99     0-5                                         Granules, Baits                                                                             0.01-95    5-99     0-15                                        and Pellets                                                                   High Strength 90-99      0-10     0-2                                         Compositions                                                                  ______________________________________                                    

Lower or higher levels of active ingredient can, of course, be presentdepending on the intended use and the physical properties of thecompound. Higher ratios of surfactant to active ingredient are sometimesdesirable, and are achieved by incorporation into the formulation or bytank mixing.

Typical solid diluents are described in Watkins, et al., "Handbook ofInsecticide Dust Diluents and Carriers", 2nd Ed., Dorland Books,Caldwell, N.J. The more absorptive diluents are preferred for wettablepowders and the denser ones for dusts. Typical liquid diluents andsolvent are described in Marsden, "Solvents Guide," 2nd Ed.,Interscience, New York, 1950. Solubility under 0.1% is preferred forsuspension concentrates; solution concentrates are preferably stableagainst phase separation at 0° C. "McCutcheon's Detergents andEmulsifiers Annual", Allured Publ. Corp., Ridgewood, N.J., as well asSisely and Wood, "Encyclopedia of Surface Active Agents", Chemical Publ.Co., Inc., New York, 1964, list surfactants and recommended uses. Allformulations can contain minor amounts of additives to reduce foam,caking, corrosion, microbiological growth, etc. Preferably, ingredientsshould be approved by the U.S. Environmental Protection Agency for theuse intended.

The methods of making such compositions are well known. Solutions areprepared by simply mixing the ingredients. Fine solid compositions aremade by blending and, usually, grinding as in a hammer or fluid energymill. Suspensions are prepared by wet milling (see, for example, U.S.Pat. No. 3,060,084). Granules and pellets can be made by spraying theactive material upon preformed granular carriers or by agglomerationtechniques. See J. E. Browning, "Agglomeration", Chemical Engineering,Dec. 4, 1967, pages 147 and following, and "Perry's Chemical Engineer'sHandbook", 4th Ed., McGraw-Hill, New York, 1963, pages 8 to 59 andfollowing.

EXAMPLE A Emulsifiable Concentrate

    ______________________________________                                        5-chloro-6-ethyl-N-[2-[4-(trimethylsilyl)phenyl]-                                                        20%                                                ethyl]-4-pyrimidinamine                                                       blend of oil soluble sulfonates                                                                          10%                                                and polyoxyethylene ethers                                                    isophorone                 70%                                                ______________________________________                                    

The ingredients are combined and stirred with gentle warming to speedsolution. A fine screen filter is included in packaging operation toinsure the absence of any extraneous undissolved material in theproduct.

EXAMPLE B Wettable Powder

    ______________________________________                                        5-chloro-6-ethyl-N-[2-(2-naphthalenyl)ethyl]-4-                                                         30%                                                 4-pyrimidinamine                                                              sodium alkylnaphthalenesulfonate                                                                         2%                                                 sodium ligninsulfonate     2%                                                 synthetic amorphous silica                                                                               3%                                                 kaolinite                 63%                                                 ______________________________________                                    

The active ingredient is mixed with the inert materials in a blender.After grinding in a hammermill, the material is re-blended and siftedthrough a 50 mesh screen.

EXAMPLE C Dust

    ______________________________________                                        Wettable powder of Example B                                                                        10%                                                     pyrophyllite (powder) 90%                                                     ______________________________________                                    

The wettable powder and the pyrophyllite diluent are thoroughly blendedand then packaged. The product is suitable for use as a dust.

EXAMPLE D Granule

    ______________________________________                                        β-[(5-chloro-6-ethyl-4-pyrimidinyl)amino]-4-                                                       10%                                                 (1,1-dimethylethyl)benzeneethanol                                             attapulgite granules (low volative                                                                      90%                                                 matter, 0.71/0.30 mm; U.S.S No.                                               25-50 sieves)                                                                 ______________________________________                                    

The active ingredient is dissolved in a volatile solvent such as acetoneand sprayed upon dedusted and pre-warmed attapulgite granules in adouble cone blender. The acetone is then driven off by heating. Thegranules are then allowed to cool and are packaged.

EXAMPLE E Granule

    ______________________________________                                        Wettable powder of Example B                                                                        15%                                                     gypsum                69%                                                     potasium sulfate      16%                                                     ______________________________________                                    

The ingredients are blended in a rotating mixer and water sprayed on toaccomplish granulation. When most of the material has reached thedesired range of 0.1 to 0.42 mm (U.S.S. No. 18 to 40 sieves), thegranules are removed, dried, and screened. Oversize material is crushedto produce additional material in the desired range. These granulescontain 4.5% active ingredient.

EXAMPLE F Solution

    ______________________________________                                        α-[(5-chloro-6-ethyl-4-pyrimidinyl)amino]-4-                                                      25%                                                 (1,1-dimethylethyl)benzeneacetamide                                           N-methyl-pyrrolidone      75%                                                 ______________________________________                                    

The ingredients are combined and stirred to produce a solution suitablefor direct, low volume application.

EXAMPLE G Aqueous Suspension

    ______________________________________                                        methyl α-[(5-chloro-6-ethyl-4-pyrimidinyl)amino]-                                                  40%                                                4-(1,1-dimethylethyl)benzeneacetate                                           polyacrylic acid thickener 0.3%                                               dodecyclophenol polyethylene glycol                                                                      0.5%                                               ether                                                                         disodium phosphate         1.0%                                               monosodium phosphate       0.5%                                               polyvinyl alcohol          1.0%                                               water                      56.7%                                              ______________________________________                                    

The ingredients are blended and ground together in a sand mill toproduce particles substantially all under 5 microns in size.

EXAMPLE H Oil Suspension

    ______________________________________                                        7-chloro-2,3,3a,4-tetrahydro-3a-oxiranyl-N-[4-                                                          35.0%                                               (trifluoromethyl)phenyl][1]benezopyarno-                                      [4,3-C]pyrazole-2-carboxamide                                                 blend of polyalchohol carboxylic                                                                         6.0%                                               esters and oil soluble petroleum                                              sulfonates                                                                    xylene range solvent      59.0%                                               ______________________________________                                    

The ingredients are combined and ground together in a sand mill toproduce particles substantially all below 5 microns. The product can beused directly, extended with oils, or emulsified in water.

EXAMPLE I Bait Granules

    ______________________________________                                        5-chloro-6-ethyl-N-[1-[4-(trimethylsilyl)phenyl]-                                                         3.0%                                              propyl]-4-pyrimidinamine                                                      blend of polyethoxylated nonyl-                                                                           9.0%                                              phenols and sodium dodecyl-                                                   benzene sulfonates                                                            ground up corn cobs        88.0%                                              ______________________________________                                    

The active ingredient and surfactant blend are dissolved in a suitablesolvent such as acetone and sprayed onto the ground corn cobs. Thegranules are then dried and packaged.

Compounds of Formula I can also be mixed with one or more otherinsecticides, fungicides, nematocides, bactericides, acaricides, orother biologically active compounds to form a multi-component pesticidegiving an even broader spectrum of effective agricultural protection.Examples of other agricultural protectants with which compounds of thisinvention can be formulated are:

Insecticides:

3-hydroxy-N-methylcrotonamide(dimethylphosphate)ester (monocrotophos)

methylcarbamic acid, ester with 2,3-dihydro-2,2-dimethyl-7-benzofuranol(carbofuran)

O-[2,4,5-trichloro-α-(chloromethyl)benzyl]phosphoric acid,O',O'-dimethyl ester (tetrachlorvinphos)

2-mercaptosuccinic acid, diethyl ester, S-ester with thionophosphoricacid, dimethyl ester (malathion)

phosphorothioic acid, O,O-dimethyl, O-p-nitrophenyl ester (methylparathion)

methylcarbamic acid, ester with α-naphthol (carbaryl)

methyl O-(methylcarbamoyl)thiolacetohydroxamate (methomyl)

N'-(4-chloro-o-tolyl)-N,N-dimethylformamidine (chlordimeform)

O,O-diethyl-O-(2-isopropyl-4-methyl-6-pyrimidylphosphorothioate(diazinon)

octachlorocamphene (toxaphene)

O-ethyl-O-p-nitrophenyl phenylphosphonothioate (EPN)

(S)-α-cyano-m-phenoxybenzyl(1R, 3R)-3-(2,2-dibromovinyl)-2,2-dimethylcyclopropanecarboxylate (deltamethrin)

Methyl-N',N'-dimethyl-N-[(methylcarbamoyl)oxy]-1 -thioox amimidate(oxamyl)

cyano (3-phenoxyphenyl)-methyl -4-chloro-a-(1-methylethyl)benzeneacetate(fenvalerate)

(3-phenoxyphenyl)methyl(+)-cis,trans-3-(2,2-dichloroethenyl)-2,2-dimethylcyclopropanecarboxylate(permethrin)

α-cyano-3-phenoxybenzyl 3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylate (cypermethrin)

O-ethyl-S-(p-chlorophenyl)ethylphosphonodithioate (profenofos)

phosphorothiolothionic acid,

O-ethyl-O-[4-(methylthio)-phenyl]-S-n-propyl ester (sulprofos).

Additional insecticides are listed hereafter by their common names:triflumuron, diflubenzuron, methoprene, buprofezin, thiodicarb,acephate, azinphosmethyl, chlorpyrifos, dimethoate, fonophos,isofenphos, methidathion, methamidiphos, monocrotphos, phosmet,phosphamidon, phosalone, pirimicarb, phorate, terbufos, trichlorfon,methoxychlor, bifenthrin, biphenate, cyfluthrin, fenpropathrin,fluvalinate, flucythrinate, tralomethrin, metaldehyde and rotenone.

Fungicides:

methyl 2-benzimidazolecarbamate (carbendazim)

tetramethylthiuram disulfide (thiuram)

n-dodecylguanidine acetate (dodine)

manganese ethylenebisdithiocarbamate (maneb)

1,4-dichloro-2,5-dimethoxybenzene (chloroneb)

methyl 1-(butylcarbamoyl)-2-benzimidazolecarbamate (benomyl)

1-[2-(2,4-dichlorophenyl)-4-propyl-1,3-dioxolan-2-yl-methyl]-1H-2,4-triazole(propiconazole)

2-cyano-N-ethylcarbamoyl-2-methoxyiminoacetamide (cymoxanil)

1-(4-chlorophenoxy)-3,3-dimethyl-1-(1H-1, 2,4-triazol-1-yl)-2-butanone(triadimefon)

N-(trichloromethylthio)tetrahydrophthalimide (captan)

N-(trichloromethylthio)phthalimide (folpet)

dimethyl 4,4'-(o-phenylene) bis (3-thioallophanate) (thiophanate-methyl)

2-(thiazol-4-yl)benzimidazole (thiabendazole)

aluminum tris (O-ethylphosphonate) (phosethyl aluminum)

tetrachloroisophthalonitrile (chlorothalonil)

2,6-dichloro-4-nitroaniline (dichloran)

N- (2,6-dimethylphenyl)-N-(methoxyacetyl)alanine methyl ester(metalaxyl)

cis-N-[1,1,2,2-tetrachloroethyl)thio]cyclohex4-ene-1,2-dicarbioximide(captafol)

3-(3,5-dichlorophenyl)-N-(2-methylethyl)-2,4-dioxolimidazolidinecarboxamide (iprodione)

3-(3,5-dichlorophenyl)-5-ethenyl-5-methyl-2,4-oxazolidinedione(vinclozolin)

kasugamycin

O-ethyl-S,S-diphenylphosphorodithioate (edifenphos)

4-(3-(4-(1,1-dimethylethyl)phenyl-2-methyl)propyl-2,6-dimethylmorpholine(fenpropimorph)

4-(3-4(1,1-dimethylethyl)phenyl)-2-methyl)propylpiperidine(fenpropidine)

2-(4-chlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)hexanenitrile(myclobutanil)

1-[2-(4-chlorophenyl)ethyl]-1-(1,1-dimethylethyl)-1-(1H-1,2,4-triazole-1-yl)ethanol(tebuconazol)

3-chloro-4-[4-methyl-2-(1H-1,2,4-triazol)-1-ylmethyl)-1,3-dioxolan-2-yl]phenyl-4-chlorophenylether (difenoconazole)

1-[2-(2,4-dichlorophenyl)pentyl]-1H-1,2,4-triazole (penconazole)

2,4'-difluoro-1-(1H-1,2,4-triazole-1-ylmethyl)benzhydryl alcohol(flutriafol)

1-[[[bis(4-fluorophenyl)]methylsilyl]methyl]-1H-1,2,4-triazole(flusilazole)

N-propyl-N-[2-(2,4,6-trichlorophenoxy)ethyl]imidazole-1-carboxamide(prochloraz)

1-[2-(2,4-dichlorophenyl)-4-propyl-1,3-dioxolan-2-ylmethyl]-1H-1,2,4-triazole(propiconazole)

1-(2-chlorophenyl)-1-(4-chlorophenyl)-1-(5-pyrimidin)methanol(fenarimol)

1-(4-chlorophenoxy)-3,3-dimethyl-1-(1H-1, 2,4-triazole-1-yl)butan-2-ol(triadimenol)

1-(2,4-dichlorophenyl)-4,4-dimethyl-2-(1H-1,2,4-triazol-1-yl)pentan-3-ol(diclobutrazol)

copper oxychloride

methyl N(2,6-dimethylphenyl)-N-(2-furanylcarbonyl)-DL-alaninate(furalaxyl)

N-(trichloromethylthio)phthalimide (folpet)

Nematocides:

S-methyl 1-(dimethylcarbamoyl)-N-(methylcarbamoyloxy)thioformimidate

S-methyl 1-carbamoyl-N-(methylcarbamoyloxy)thioformimidate

N-isopropylphosphoramidic acid O-ethylO'-[4-(methylthio)-m-tolyl]diester (fenamiphos)

Bactericides:

tribasic copper sulfate

streptomycin sulfate

Acaricides:

senecioic acid, ester with 2-sec-butyl-4,6-dinitrophenol (binapacryl)

6-methyl-1,3-cithiolo[4,5-β]quinoxalin-2-one (oxythioquinox)

ethyl 4,4'-dichlorobenzilate (chlorobenzilate)

1,1-bis(p-chlorophenyl)-2,2,2-trichloroethanol (dicofol)

bis(pentachloro-2,4-cyclopentadien-1-yl) (dienochlor)

tricyclohexyltin hydroxide (cyhexatin)

trans-5-(4-chlorophenyl)-N-cyclohexyl-4-methyl-2-oxothiazolidine-3-carboxamide(hexythiazox)

amitraz

propargite

fenbutatin-oxide

Biological

Bacillus thuringiensis

Avermectin B.

Utility

The compounds of this invention are useful against agronomic andnonagronomic pests. They exhibit activity against a wide spectrum offoliar and soil inhabiting arthropods which are pests of growing andstored agronomic crops, forestry, greenhouse crops, ornamentals, nurserycrops, stored food and fiber products, livestock, household, and publicand animal health. Those skilled in the art will recognize that not allcompounds are equally effective against all pests but the compounds ofthis invention display activity against economically importantagronomic, forestry, greenhouse, ornamental food and fiber product,stored product, domestic structure, and nursery pests, such as:

larvae of the order Lepidoptera including fall and beet armyworm andother Spodoptera spp., tobacco budworm, corn earworm and other Heliothisspp., European corn borer, navel orangeworm, stalk/stem borers and otherpyralids, cabbage and soybean loopers and other loopers, codling moth,grape berry moth and other tortricids, black cutworm, spotted cutworm,other cutworms and other noctuids, diamondback moth, green cloverworm,velvetbean caterpillar, green cloverworm, pink bollworm, gypsy moth, andspruce budworm;

foliar feeding larvae and adults of the order Coleoptera includingColorado potato beetle, Mexican bean beetle, flea beetle, Japanesebeetles, and other leaf beetles, boll weevil, rice water weevil, granaryweevil, rice weevil and other weevil pests, and soil inhabiting insectssuch as Western corn rootworm and other Diabrotica spp., Japanesebeetle, European chafer and other coleopteran grubs, and wireworms;

adults and larvae of the orders Hemiptera and Homoptera includingtarnished plant bug and other plant bugs (miridae), aster leafhopper andother leafhoppers (cicadellidae), rice planthopper, brown planthopper,and other planthoppers (fulgoroidea), psylids, whiteflies (aleurodidae),aphids (aphidae), scales (coccidae and diaspididae), lace bugs(tingidae), stink bugs (pentatomidae), cinch bugs and other seed bugs(lygaeidae), cicadas (cicadidae), spittlebugs (cercopids), squash bugs(coreidae), red bugs and cotton stainers (pyrrhocoridae);

adults and larvae of the order acari (mites) including European redmite, two spotted spider mite, rust mites, McDaniel mite, and foliarfeeding mites;

adults and inunatures of the order Orthoptera including grasshoppers;

adults and inunatures of the order Diptera including leafminers, midges,fruit flies (tephritidae), and soil maggots;

adults and immatures of the order Thysanoptera including onion thripsand other foliar feeding thrips.

The compounds are also active against economically important livestock,household, public and animal health pests such as:

insect pests of the order Hymenoptera including carpenter ants, bees,hornets, and wasps;

insect pests of the order Diptera including house flies, stable flies,face flies, horn flies, blow flies, and other muscoid fly pests, horseflies, deer flies and other Brachycera, mosquitoes, black flies, bitingmidges, sand flies, sciarids, and other Nematocera;

insect pests of the order Orthoptera including cockroaches and crickets;

insect pests of the order Isoptera including the Eastern subterraneantermite and other termites;

insect pests of the order Mallophaga and Anoplura including the headlouse, body louse, chicken head louse and other sucking and chewingparasitic lice that attack man and animals;

insect pests of the order Siphonoptera including the cat flea, dog fleaand other fleas.

Finally, the compounds of this invention are useful as plant diseasecontrol agents. They provide control of diseases caused by a broadspectrum of fungal plant pathogens in the Basidiomycete, Ascomycete andOomycete classes. They are effective in controlling a broad spectrum ofplant diseases, particularly foliar pathogens of ornamental, vegetable,field, cereal, and fruit crops. These pathogens include, Venturiainaequalis, Cercosporidium personatum, Cercospora arachidicola,Cercospora beticola, Pseudocercosporella herpotrichoides, Erysiphegraminis, Uncinula necatur, Podosphaera leucotricha, Puccinia recondita,Puccinia gramminis, Hemileia vastatrix, Puccinia striiformis, Pucciniaarachidis, Pyricularia oryzae, Phytophthora infestaris, Plasmoparaviticola, Peronospora tabacina, Pseudoperonospora cubensis, Pythiumaphanidermatum and other species closely related to these pathogens.They also control seed pathogens.

The specific species for which arthropod control is exemplified are:fall armyworm, Spodoptera fruigiperda; tobacco budworm, Heliothisvirescens (Helicoverpa); boll weevil, Anthonomus grandis; asterleafhopper, Macrosteles fascifrons; black bean aphid, (Aphis Fabae);southern corn rootworm, Diabrotica undecimpunctata and two-spottedspider mite (Tetranychus urt). The pest control protection afforded bythe compounds of the present invention is not limited, however, to thesespecies. The compounds of this invention may also be utilized asrodenticides.

The specific plant pathogens for which control is exemplified are:Ventura inaequalis (the causal agent of apple scab); Cercosporidiumpersonatum (the causal agent of peanut late leafspot); Erysiphe graminisf. sp. tritici (the causal agent of wheat powdery mildew); Pucciniacecondita (the causal agent of wheat leaf rust); and Plasmopara viticola(the causal agent of grape downey mildew). The plant pathogen controlprotection afforded by the compounds of the present invention is notlimited, however, to these species.

Application

Arthropod pests are controlled and protection of agronomic crops, animaland human health is achieved by applying one or more of the Formula Icompounds of this invention, in an effective amount, to the environmentof the pests including the agronomic and/or nonagronomic locus ofinfestation, to the area to be protected, or directly on the pests to becontrolled. Because of the diversity of habitat and behavior of thesearthropod pest species, many different methods of application areemployed. A preferred method of application is by spraying withequipment that distributes the compound in the environment of the pests,on the foliage, animal, person, or premise, in the soil or animal, tothe plant part that is infested or needs to be protected. Alternatively,granular formulations of these toxicant compounds can be applied to orincorporated into the soil. Other methods of application can also beemployed including direct and residual sprays, aerial sprays, baits,eartags, boluses, foggets, aerosols, and many others. The compounds canbe incorporated into baits that are consumed by the arthropods or indevices such as traps and the like which entice them to ingest orotherwise contact the compounds.

Plant disease control is ordinarily accomplished by applying aneffective amount of the compound either preinfection or post-infectionto the portion of the plant to be protected such as the roots, stems,foliage, fruit, seeds, tubers or bulbs, or to the media (soil or sand)in which the plants to be protected are growing. The compound may alsobe applied to the seed, to protect the seed and seedling.

The compounds of this invention can be applied in their pure state, butmost often application will be of a formulation comprising one or morecompounds with suitable carriers, diluents, and surfactants and possiblyin combination with a food depending on the contemplated end use. Apreferred method of application involves spraying a water dispersion orrefined oil solution of the compounds. Combinations with spray oils,spray oil concentrations, and synergists such as piperonyl butoxideoften enhance the efficacy of the compounds of Formula I.

The rate of application of the Formula I compounds required foreffective arthropod control will depend on such factors as the speciesof arthropod to be controlled, the pest's life cycle, life stage, itssize, location, time of year, host crop or animal, feeding behavior,mating behavior, ambient moisture, temperature, etc. In general,application rates of 0.01 to 2 kg of active ingredient per hectare aresufficient to provide large-scale effective control of pests inagronomic ecosystems under normal circumstances, but as little as 0.001kg/hectare or as much as 8 kg hectare may be required. For nonagronomicapplications, effective use rates will range from about 1.0 to 50mg/square meter but as little as about 0.1 mg/square meter or as much as150 mg/square meter may be required.

Rates of application for these compounds as plant disease control agentscan be influenced by many factors of the environment and should bedetermined under actual use conditions. Foliage can normally beprotected when treated at a rate of from less than 10 g/ha to 10,000g/ha of active ingredient. Plants growing in soil treated at aconcentration from 0.1 to about 20 kg/ha can be protected from disease.Seed and seedlings can normally be protected when seed is treated at arate of from 0.1 to 10 g per kilogram of seed.

The following tests demonstrate the control efficacy of compounds ofFormula I on specific pests and plant pathogens; see Index Tables A andB for compound descriptions. Compounds for which no data are reportedwere either not screened or have activities lower than the recitedminimum values.

    __________________________________________________________________________    INDEX TABLE A                                                                  ##STR28##                                                                    CMPD                                                                              R.sup.5 A             R.sup.6    mp (°C.)                          __________________________________________________________________________     1  H       CHC(O)NH.sub.2                                                                              4-tBu      glass.sup.a                               2  H       CHCO.sub.2 Me 4-tBu      wax.sup.b                                 3  H       CHCO.sub.2 H  4-tBu      solid.sup.c                               4  H       CHCO.sub.2 Me 3-O-(4-F-Ph)                                                                             oil.sup.d                                 5  H       CHC(O)NH.sub.2                                                                              3-O-(4-F-Ph)                                                                             oil.sup.e                                 6  H       CHCH.sub.2 OH 4-tBu      118-120                                   7  H       CH(CO.sub.2 Me)CH.sub.2                                                                     4-tBu      oil.sup.f                                 8  H       CH.sub.2 CH.sub.2                                                                           4-SiMe.sub.3                                                                             101-103                                   9  H       CHEt          4-SiMe.sub.3                                                                             oil.sup.g                                10  H       CHCMe.sub.2 (OH)                                                                            4-tBu      158-160                                  11  H       CH(CO.sub.2 Me)CH.sub.2                                                                     4-F        75-78                                    12  H       CH.sub.2 CH.sub.2                                                                           4-SiMe.sub.2 (tBu)                                                                       110-112                                  13  H       CHCHMe(OH)    4-tBu      wax.sup.h                                14  H       CHCH.sub.2 OC(O)Me                                                                          4-tBu      oil.sup.i                                15  H       CH(CH.sub.2 OH)CH.sub.2                                                                     4-tBu      128-13O                                  16  H       CH(CO.sub.2 Bu)CH.sub.2                                                                     4-F        oil.sup.j                                17  H       CHCH.sub.2 OCMe.sub.2 (OMe)                                                                 4-tBu      oil.sup.k                                18  H       CHiPr         4-SiMe.sub.3                                                                             oil.sup.l                                19  C(O)imidazole                                                                         CH.sub.2 CH.sub.2                                                                           4-SiMe.sub.3                                                                             oil.sup.m                                20  H       CH.sub.2 CH.sub.2                                                                           4-SiMe.sub.3                                                                             184-186 (HCl salt)                       21  H       CH.sub.2 CH.sub.2                                                                           4-SiEt3    77-79                                    22  H       CH.sub.2 CH.sub.2                                                                           4-SiMe.sub.2 (Ph)                                                                        71-73                                    23  H       CHCH.sub.2 OCH.sub.2 CH.sub.2 OEt                                                           4-tBu      oil.sup.n                                24  H       CHMe          4-SiMe.sub.3                                                                             78-80                                    25  H       CHCO.sub.2 CH.sub.2 CH.sub.2 OMe                                                            4-tBu      oil.sup.o                                26  H       CH(Me)CH(OSiMe.sub.3)                                                                       4-tBu      oil.sup.p                                27  H       CH(Me)CH(OSiMe.sub.3)                                                                       4-tBu      oil.sup.q                                28  H       CHCO.sub.2 C.sub.7 H.sub.15                                                                 4-tBu      oil.sup.r                                29  H       CH.sub.2 CH(Me)CH(OSiMe.sub.3)                                                              4-tBu      oil.sup.s                                30  H       CHCH.sub.2 OC(O)Bu                                                                          4-tBu      oil.sup.t                                31  H       CH(CO.sub.2 CH.sub.2 Ph)CH.sub.2                                                            4-tBu      94-97                                    32  H       CHCH.sub.2 OCH.sub.2 Ph                                                                     4-tBu      oil.sup.u                                33  H       CH.sub.2 CH(Me)CH(OH)                                                                       4-tBu      107-110                                  34  H       CH(Me)CH(OH)  4-tBu      glass.sup.v                              35  H       CH(Me)CH(OH)  4-tBu      glass.sup.w                              36  H       CH[CH.sub.2 OC(O)Me]CH.sub.2                                                                4-tBu      oil.sup.x                                37  H       CH[CH.sub.2 OCMe.sub.2 (OMe)]CH.sub.2                                                       4-tBu      oil.sup.y                                38  Me      CH.sub.2 CH.sub.2                                                                           4-SiMe.sub.3                                                                             oil.sup.z                                39  H       CH(CH.sub.2 OCH.sub.2 Ph)CH.sub.2                                                           4-tBu      oil.sup.aa                               40  H       CH.sub.2 CH.sub.2                                                                           3-SiMe.sub.3                                                                             93-95                                    41  H       CHMe          4-SiMe.sub.3                                                                             196-199 (HCl salt)                       42  H       CHCN          4-tBu      wax.sup.bb                               43  H       CHMe          4-SiMe.sub.3                                                                             [α].sub.D.sup.25 = +15.9           44  H       CHMe          4-SiMe.sub.3                                                                             [α].sub.D.sup.25 = -13.9           45  H       CHCN          3-O-(4-F-Ph)                                                                             glass.sup.cc                             46  H       CHCH.sub.2 OCH.sub.2 CF.sub.3                                                               4-tBu      oil.sup.dd                               47  H       CH.sub.2 CH.sub.2                                                                           4-CO.sub.2 Et                                                                            134-135                                  48  H       CH.sub.2 CH.sub.2                                                                           4-CO.sub.2 CH.sub.2 CF.sub.3                                                             oil                                      49  H       CHMe          4-CO.sub.2 Et                                                                            101-102                                  50  H       CH.sub.2 CH.sub.2                                                                           4-CO.sub.2 Me                                                                            138-139                                  51  H       CH.sub.2 CH.sub.2                                                                           4-C(O)Ph   wax.sup.ee                               52  H       CH.sub.2 CH.sub.2                                                                           4-C(O)iPr  oil.sup.ff                               53  H       CH.sub.2 CH.sub.2                                                                           4-C(O)Et   116-118                                  54  H       CH.sub.2 CH.sub.2                                                                           4-C(O)(4-ClPh)                                                                           oil.sup.gg                               55  H       CH.sub.2 CH.sub.2                                                                           4-C(O)nPr  104-107                                  56  H       CH.sub.2 CH.sub.2                                                                           4-C(O)(.sub.2 -ClPh)                                                                     oil.sup.hh                               57  H       CH.sub.2 CH.sub.2                                                                           4-C(O)(3-ClPh)                                                                           99-101                                   58  H       CH.sub.2 CH.sub.2                                                                           4-C(O)(4-FPh)                                                                            109-110                                  59  H       CH.sub.2 CH.sub.2                                                                           4-C(O)(2,4-di-ClPh)                                                                      oil.sup.ii                               60  H       CH.sub.2 CH.sub.2                                                                           4-C(O)(3,5-di-ClPh)                                                                      wax.sup.jj                               61  H       CH.sub.2 CH.sub.2                                                                           4-C(O)Me   94-96                                    62  H       CH.sub.2 CH.sub.2                                                                           4-C(O)(2,4-di-FPh)                                                                       95-97                                    63  H       CH.sub.2 CH.sub.2                                                                           4-C(O)CH.sub.2 Ph                                                                        oil.sup.kk                               64  H       CH.sub.2 CH.sub.2                                                                           4-C(O)(3,4-di-FPh)                                                                       oil.sup.ll                               65  H       CH.sub.2 CH.sub.2                                                                           4-C(O)iBu  oil                                      66  H       CH.sub.2 CH.sub.2                                                                           4-CO.sub.2 iPr                                                                           105-106                                  78  H       CHMe          4-GeMe.sub.3                                                                             74-77                                    __________________________________________________________________________

                  INDEX TABLE B                                                   ______________________________________                                         ##STR29##                                                                    CMPD  R.sup.5                                                                              A        Q               mp (°C.)                         ______________________________________                                        67    H      CH.sub.2                                                                                ##STR30##      oil.sup.mm                              68    H      CH.sub.2                                                                                ##STR31##      oil.sup.nn                              69    H      CH.sub.2 CH.sub.2                                                                       ##STR32##      92-95                                   70    H      CH.sub.2 CH.sub.2                                                                       ##STR33##      79-83                                   71    Et     CH.sub.2                                                                                ##STR34##      oil.sup.oo                              72    Me     CH.sub.2                                                                                ##STR35##      oil.sup.pp                              73    H      CHEt                                                                                    ##STR36##      oil.sup.qq                              74    H      CHMe                                                                                    ##STR37##      79-82                                   75    H      CHMe                                                                                    ##STR38##      96-98                                   76    H      CHMe                                                                                    ##STR39##      83-86                                   77    H      CHMe                                                                                    ##STR40##      oil.sup.rr                              ______________________________________                                    

¹ HNMR

^(a) (CDCl₃): δ 8.39 (s, 1H), 7.41 (s, 4H), 6.60 (brd, 1H), 5.69 (brs,2H), 5.63 (d, 1H), 2.78 (q, 2H), 1.31 (s, 9H), 1.24 (t, 3H).

^(b) (CDCl₃): δ 8.40 (s, 1H), 7.39 (s, 4H), 6.22 (brd, 1H), 5.73 (d,1H), 3.76 (s, 3H), 2.80 (q, 2H), 1.31 (s, 9H), 1.25 (t, 3H).

^(c) (DMSO-d₆): δ 8.33 (s, 1H), 7.37 (s, 4H), 7.10 (d, 1H), 5.60 (d,1H), 3.30 (brs, 1H), 2.72 (q, 2H), 1.25 (s, 9H), 1.15 (t, 3H).

^(d) (CDCl₃): δ 8.38 (s, 1H), 7.32 (m, 2H), 7.20-6.05 (m, 6H), 6.33(brd, 1H), 5.74 (d, 1H), 3.77 (s, 3H), 2.80 (q, 2H), 1.26 (t, 3H).

^(e) (CDCl₃): δ 8.28 (s, 1H), 7.40-6.85 (m, 8H), 6.66 (d, 1H), 5.67(brd, 1H), 5.60 (d, 1H), 2.80 (q, 2H), 1.25 (t, 3H).

^(f) (CDCl₃): δ 8.40 (s, 1H), 7.30, 7.08 (ABq, 4H), 5.78 (brd, 1H), 5.06(q, 1H), 3.75 (s, 3H), 3.19 (m, 2H), 2.78 (q, 2H), 1.30 (s, 9H), 1.25(t, 3H).

^(g) (CDCl₃): δ 8.38 (s, 1H), 7.49, 7.32 (ABq, 4H), 5.65 (brd, 1H), 5.15(q, 1H), 2.78 (q, 2H), 1.93 (m, 2H), 1.25 (t, 3H), 0.96 (t, 3H), 0.26(s, 9H).

^(h) (CDCl₃): δ 8.35 (s, 1H), 7.38, 7.32 (ABq, 4H), 6.26 (brd, 1H), 5.19(m, 1H), 4.20 (m, 1H), 2.79 (q, 2H), 2.32 (brd, 1H), 1.31 (s, 9H), 1.28(t, 3H), 1.17 (d, 3H).

^(i) (CDCl₃): δ 8.40 (s, 1H), 7.39, 7.30 (ABq, 4H), 5.98 (brd, 1H), 5.55(m, 1H), 4.42 (d, 2H), 2.79 (q, 2H), 2.05 (s, 3H), 1.31 (s, 9H), 1.26(t, 3H).

^(j) (CDCl₃): δ 8.41 (s, 1H), 7.10 (m, 2H, 7.00 (m, 2H), 5.82 (d, 1H),5.05 (q, 1H), 4.12 (m, 2H), 3.19 (d, 2H), 2.80 (q, 2H), 1.58 (m, 2H),1.26 (m, 5H), 0.91 (t, 3H).

^(k) (CDCl₃): δ 8.36 (s, 1H), 7.34, 7.31 (ABq, 4H), 6.18 (brd, 1H), 5.37(m, 1H), 3.75 (m, 2H), 3.03 (s, 3H), 2.80 (q, 2H), 1.30 (m, 18H).

^(l) (CDCl₃): δ 8.35 (s, 1H), 7.47, 7.27 (ABq, 4H), 5.78 (d, 1H), 5.06(t, 1H), 2.77 (q, 2H), 2.18 (m, 1H), 1.24 (t, 3H), 1.00 (d, 3H), 0.92(d, 3H), 0.24 (s, 9H).

^(m) (CDCl₃): δ 8.68 (s, 1H), 7.63 (s, 1H), 7.38, 7.17 (ABq, 4H), 6.88(s, 2H), 4.25 (t, 2H), 3.06 (t, 2H), 2.82 (q, 2H), 1.20 (t, 3H), 0.23(s, 9H).

^(n) (CDCl₃): δ 8.34 (s, 1H), 7.35, 7.30 (ABq, 4H), 6.18 (d, 1H), 5.40(q, 1H), 3.85 (m, 2H), 3.70-3.45 (m, 4H), 2.78 (q, 2H), 1.30 (s, 9H),1.21 (m, 6H).

^(o) (CDCl₃): δ 8.40 (s, 1H), 7.40 (s, 4H), 6.14 (brd, 1H), 5.97 (d,1H), 4.30 (m, 2H), 3.55 (t, 2H), 3.28 (s, 3H), 2.80 (q, 2H), 1.31 (s,9H), 1.25 (t, 3H).

^(p) (CDCl₃): δ 8.43 (s, 1H), 8.30, 8.25 (ABq, 4H), 5.65 (brd, 1H), 4.96(d, 1H), 4.42 (m, 1H), 2.80 (q, 2H), 1.32 (s, 9H), 1.27 (t, 3H), 0.98(d, 3H), 0.45 (s, 9H), single diastereomer

^(q) (CDCl₃): δ 8.25 (s, 1H), 7.24, 7.18 (ABq, 4H), 5.72 (brd, 1H), 4.73(d, 1H), 4.36 (m, 1H), 2.76 (q, 2H), 1.27 (s, 9H), 1.23 (m, 6H), 0.92(s, 9H), single diastereomer

^(r) (CDCl₃): δ 8.40 (s, 1H), 7.39 (s, 4H), 6.28 (brd, 1H), 5.72 (d,1H), 4.16 (m, 2H), 2.80 (q, 2H), 1.60 (m, 2H), 1.32 (s, 9H), 1.15 (m,9H), 0.85 (m, 5H).

^(s) (CDCl₃): δ 8.30 (s, 1H), 7.26, 7.13 (ABq, 4H), 6.35 (m, 1H), 4.70(d, 1H), 4.60 (d, 1H), 3.40 (m, 2H), 2.73 (q, 2H), 2.18 (m, 1H), 2.00(m, 1H), 1.25 (s, 9H), 1.21 (t, 3H), 0.98 (d, 3H), 0.82 (d, 3H), 0.00(s, 9H), mixture of diastereomers

^(t) (CDCl₃): δ 8.39 (s, 1H), 7.38, 7.30 (ABq, 4H), 5.98 (brd, 1H), 5.58(m, 1H), 4.55 (dd, 1H), 4.35 (dd, 1H), 2.79 (q, 2H), 2.29 (t, 2H),1.65-1.45 (m, 2H), 1.31 (s, 9H), 1.26 (m, 5H), 0.84 (t, 3H).

^(u) (CDCl₃): δ 8.35 (s, 1H), 7.40-7.20 (m, 9H), 6.13 (d, 1H), 5.42 (m,1H), 4.56 (s, 2H), 3.80 (m, 2H), 2.79 (q, 2H), 1.30 (s, 9H), 1.29 (t,3H).

^(v) (CDCl₃): δ 8.41 (s, 1H), 7.38, 7.10 (ABq, 4H), 7.49 (d, 1H), 4.95(m, 1H), 4.59 (m, 1H), 3.65 (d, 1H), 2.80 (q, 2H), 1.32 (s, 9H), 1.27(t, 3H), 1.13 (d, 3H), single diastereomer

^(w) (CDCl₃): δ 8.34 (s, 1H), 7.35, 7.28 (ABq, 4H), 5.60 (d, 1H), 4.69(t, 1H), 4.45 (m, 1H), 3.38 (d, 1H), 2.78 (q, 2H), 1.30 (s, 9H), 1.23(m, 6H), single diastereomer

^(x) (CDCl₃): δ 8.42 (s, 1H), 7.32, 7.16 (ABq, 4H), 5.54 (d, 1H), 4.70(brm, 1H), 4.16 (d, 2H), 3.05-2.85 (m, 2H), 2.79 (q, 2H), 2.09 (s, 3H),1.30 (s, 9H), 1.26 (t, 3H).

^(y) (CDCl₃): δ 8.40 (s, 1H), 7.30, 7.18 (ABq, 4H), 5.78 (brd, 1H), 4.55(brm, 1H), 3.45 (d, 2H), 3.20 (d, 3H), 2.95 (m, 2H ), 2.78 (q, 2H),1.40-1.20 (m, 18H).

^(z) (CDCl₃): δ 8.43 (s, 1H), 7.45, 7.22 (ABq, 4H), 3.78 (m, 2H), 3.18(s, 3H), 2.96 (m, 2H), 2.84 (q, 2H), 1.27 (t, 3H), 0.25 (s, 9H).

^(aa) (CDCl₃): δ 8.40 (s, 1H), 7.34 (m, 5H), 7.28, 7.14 (ABq, 4H), 5.77(d, 1H), 4.56 (s, 2H), 4.50 (brm, 1H), 3.50 (m, 2H), 2.95 (m, 2H), 2.78(q, 2H), 1.30 (s, 9H), 1.26 (t, 3H).

^(bb) (CDCl₃): δ 8.58 (s, 1H), 7.50 (s, 4H), 6.30 (d, 1H), 5.65 (brd,1H), 2.84 (q, 2H), 1.34 (s, 9H), 1.28 (t, 3H).

^(cc) (CDCl₃): δ 8.56 (s, 1H), 7.45-6.95 (m, 8H), 6.35 (d, 1H), 5.68(brd, 1H), 2.84 (q, 2H), 1.29 (t, 3H).

^(dd) (CDCl₃): δ 8.39 (s, 1H), 7.42, 7.28 (ABq, 4H), 5.90 (brm, 1H),4.62 (m, 1H), 4.03 (m, 1H), 3.90-3.22 (brm, 3H), 2.81 (q, 2H), 1.33 (s,9H), 1.27 (t, 3H).

^(ee) (CDCl₃): δ 8.45 (s, 1H), 7.80-7.30 (m, 10H), 5.45 (s, 1H), 3.84(m, 2H), 3.07 (m, 2H), 2.80 (m, 2H), 1.30 (m, 3H).

^(ff) (CDCl₃): δ 8.45 (s, 1H), 7.90, 7.30 (ABq, 4H), 3.80 (t, 2H), 3.50(m, 1H), 3.00 (t, 2H), 2.80 (q, 2H), 1.20 (m, 9H).

^(gg) (CDCl₃): δ 8.50 (s, 1H), 7.70-7.30 (m, 8H), 5.60 (s, 1H), 3.80 (t,2H), 3.00 (t, 2H), 2.80 (q, 2H), 1.30 (t, 3H).

^(hh) (CDCl₃): δ 8.45 (s, 1H), 7.80 (m, 2H), 7.40 (m, 6H), 5.50 (s, 1H),3.80 (t, 2H), 3.00 (t, 2H), 2.80 (q, 2H), 1.30 (t, 3H).

^(ii) (CDCl₃): δ 8.50 (s, 1H), 7.80-7.20 (m, 7H), 5.45 (s, 1H), 3.80 (t,2H), 3.10 (t, 2H), 2.80 (q, 2H), 1.20 (t, 3H).

^(jj) (CDCl₃): 8.45 (s, 1H), 7.80-7.20 (m, 7H), 5.40 (s, 1H), 3.80 (t,2H), 3.10 (t, 2H), 2.80 (q, 2H), 1.25 (t, 3H).

^(kk) (CDCl₃): δ 8.40 (s, 1H), 8.00 (m, 2H), 7.20 (m, 7H), 5.40 (s, 1H),4.30 (t, 2H), 3.90 (t, 2H), 2.90 (s, 2H), 2.70 (q, 2H), 1.20 (t, 3H).

^(ll) (CDCl₃): δ 8.45 (s, 1H), 7.70-7.20 (m, 7H), 5.50 (s, 1H), 3.80 (t,2H), 3.00 (t, 2H), 2.80 (q, 2H), 1.26 (t, 3H).

^(mm) (CDCl₃): δ 8.43 (s, 1H), 6.95-6.80 (m, 3H), 5.80 (brs, 1H), 4.40(m, 1H), 4.30 (m, 1H), 4.05-3.70 (m, 3H), 2.80 (q, 2H), 1.28 (s, 9H),1.27 (t, 3H), mixture of 6-tBu and 7-tBu isomers

^(nn) (CDCl₃): δ 8.42 (s, 1H), 7.20-7.00 (m, 3H), 5.55 (brs, 1H), 3.55(t, 2H), 2.86 (m, 3H), 2.81 (q, 2H), 2.60-2.25 (m, 1H), 2.05 (brm, 2H),1.60-1.35 (brm, 1H), 1.30 (s, 9H), 1.27 (t, 3H).

^(oo) (CDCl₃): δ 8.48 (s, 1H), 7.80 (m, 4H), 7.46 (m, 3H), 5.00 (s, 2H),3.65 (q, 2H), 2.86 (q, 2H), 1.27 (m, 6H).

^(pp) (CDCl₃): δ 8.51 (s, 1H), 7.90 (m, 2H), 7.82 (m, 1H), 7.49 (m, 4H),5.26 (s, 2H), 3.16 (s, 3H), 2.87 (q, 2H), 1.29 (t, 3H).

^(qq) (CDCl₃): δ 8.38 (s, 1H), 7.82 (m, 4H), 7.46 (m, 3H), 5.73 (brd,1H), 5.30 (q, 1H), 2.77 (q, 2H), 2.03 (m, 2H), 1.25 (t, 3H), 0.99 (t,3H).

^(rr) (CDCl₃): δ 8.40 (s, 1H), 7.85 (d, 1H),7.82 (d, 1H), 7.45 (d, 1H),7.35 (d, 1H), 7.33 (s, 1H), 5.65 (brd, 1H), 5.58 (m, 1H), 2.79 (q, 2H),1.66 (d, 3H), 1.26 (t, 3H).

EXAMPLE J

Fall Armyworm

Test units, each consisting of an 8-ounce (230 mL) plastic cupcontaining a layer of wheat germ diet, approximately 0.5 cm thick, wereprepared. Five third-instar larvae of fall armyworm (Spodopterafrugiperda) were placed into each cup. Solutions of each of the testcompounds (acetone/distilled water 75/25 solvent) were sprayed into thecups. Spraying was accomplished by passing the cups, on a conveyer belt,directly beneath a flat fan hydraulic nozzle which discharged the sprayat a rate of 0.5 pounds of active ingredient per acre (about 0.55 kg/ha)at 30 p.s.i. (207 kPa). The cups were then covered and held at 27° C.and 50% relative humidity for 72 hours, after which time readings weretaken. Of the compounds tested, the following gave mortality levels of80% or higher: 8, 14, 20, 30, 40, 41, 54, 56, 57, 58, 59, 60, 62, 63,64, 65, 66, 68.

EXAMPLE K

Tobacco Budworm

The test procedure of Example J was repeated for efficacy againstthird-instar larvae of the tobacco budworm (Heliothis virescens[Helicoverpa]) except thatmortality was assessed at 48 hours. Of thecompounds tested, the following gave mortality level of 80% or higher:8, 30, 47, 54, 55, 58, 59, 62, 63, 66, 68, 70.

EXAMPLE L

Southern Corn Rootworm

The units, each consisting of an 8-ounce (230 mL) plastic cup containing1 sprouted corn seed, were prepared. The test units were sprayed asdescribed in Example J with individual solutions of the test compounds.After the spray on the cups had dried, five third-instar larvae of thesouthern corn rootworm (Diabrotica undecimpunctata howardi) were placedinto each cup. A moistened dental wick was inserted into each cup toprevent drying and the cups were then covered. The cups were then heldat 27° C. and 50% relative humidity for 48 hours, after which timemortality readings were taken. Of the compounds tested, the followinggave mortality levels of 80% or higher: 4, 5, 9, 11, 14, 15, 18, 21, 22,24, 32, 36, 40, 41, 47, 52, 53, 54, 55, 56, 57, 58, 59, 61, 62, 63, 64,66, 69, 72, 73, 74, 76.

EXAMPLE M

Aster Leafhopper

Test units were prepared from a series of 12-ounce (350 mL) cups, eachcontaining oat (Avena sativa) seedlings in a 1-inch (2.54 cm) layer ofsterilized soil. The test units were sprayed as described in Example Jwith individual solutions of the below-listed compounds. After the oatshad dried from the spraying, between 10 and 15 adult aster leafhoppers(Macrosteles quadrilineatus) were aspirated into each of the coveredcups. The cups were held at 27° C. and 50% relative humidity for 48hours, after which time mortality readings were taken. Of the compoundstested, the following gave mortality levels of 80% or higher: 2, 7, 8,9, 11, 18, 20, 24, 38, 40, 41, 49, 50, 52, 54, 57, 58, 59, 60, 61, 62,63, 64, 66, 68, 73, 74, 75, 76.

EXAMPLE N

Boll Weevil

Five adult boll weevils (Anthonomus grandis grandis) were placed intoeach of a series of 9 ounce (260 mL) cups. The test procedure employedwas then otherwise the same as in Example J. Mortality readings weretaken 48 hours after treatment. Of the compounds tested, the followinggave mortality levels of 80% or higher: 4, 8, 11, 20, 30, 38, 47, 54,56, 57, 58, 59, 62, 64, 66, 68, 70, 73, 74.

EXAMPLE O

Black Bean Aphid

Individual nasturtium leaves were infested with 5 to 10 aphids (allstages of Aphis fabae) and sprayed with their undersides facing up on ahydraulic sprayer as described in Example J. The leaves were then set ina 15×45 mm shell vial containing sugar water solution and covered with aclear plastic 1 oz (29.57 milliliters) portion cup to prevent escape ofaphids that drop from the leaves. The test units were held at 27° C. and50% relative humidity for 48 hours, after which time mortality readingswere taken. Of the compounds tested, the following gave mortality levelsof 80% or higher: 1, 2, 4, 6, 7, 8, 9, 11, 14, 15, 17, 18, 19, 20, 21,22, 24, 25, 30, 36, 37, 38, 39, 40, 41, 47, 49, 50, 51, 52, 53, 54, 55,56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 74,75, 76,78.

EXAMPLE P

Two-Spotted Spider Mite

One inch squares (2.54 centimeters) of kidney bean leaves that have beeninfested on the undersides with 25 to 30 adult mites (Tetranychusurticae) were sprayed with their undersides facing up on a hydraulicsprayer as described in Example J. The leaf squares were placedunderside up on a square of wet cotton in a petri dish and the perimeterof the leaf square was tamped down onto the cotton with forceps so thatthe mites cannot escape onto untreated leaf surface. The test units wereheld at 27° C. and 50% relative humidity for 48 hours, after which timemortality readings were taken. Of the compounds tested, the followinggave levels of 80% or higher: 1, 2, 4, 5, 6, 7, 8, 9, 11, 12, 13, 14,15, 17, 18, 19, 20, 21, 22, 24, 30, 36, 37, 38, 39, 40, 41, 42, 44, 51,52, 54, 56, 57, 58, 59, 60, 62, 63, 64, 65, 67, 68, 69, 70, 73, 74, 75,76, 78.

EXAMPLE Q

The test compounds were dissolved in acetone in an amount equal to 3% ofthe final volume and then suspended at a concentration of 200 ppm inpurified water containing 250 ppm of the surfactant Trem 14 (polyhydricalcohol esters). This suspension was sprayed to the point of run-off onwheat seedlings. The following day the seedlings were inoculated with aspore dust of Erysiphe graminis f. sp. tritici (the causal agent ofwheat powdery mildew) and incubated growth chamber at 20° C. for 7 days,after which disease ratings were made. Of the compounds tested, thefollowing gave 70% disease control or higher: 7, 8, 9, 11, 12, 14, 15,16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 29, 30, 32, 33, 35, 36,37, 38, 39, 40, 41, 49, 50, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62,65, 67, 68, 70, 71, 72, 73, 74, 75, 76, 78.

EXAMPLE R

The test compounds were dissolved in acetone in an amount equal to 3% ofthe final volume and then suspended at a concentration of 200 ppm inpurified water containing 250 ppm of the surfactant Trem 14 (polyhydricalcohol esters). This suspension was sprayed to the point of run-off onwheat seedlings. The following day the seedlings were inoculated with aspore suspension of Puccinia recondita (the causal agent of wheat leafrust) and incubated in a saturated atmosphere at 20° C. for 24 hours,and then moved to a growth chamber at 20° C. for 6 days, after whichdisease ratings were made. Of the compounds tested, the following gave70% disease control or higher: 6, 7, 8, 9, 11, 14, 15, 17, 18, 19, 20,21, 22, 23, 24, 25, 30, 36, 37, 38, 40, 41, 42, 45, 48, 49, 50, 51, 52,53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 65, 66, 67, 68, 70, 72, 73, 74,75, 76, 78.

EXAMPLE S

The test compounds were dissolved in acetone in an amount equal to 3% ofthe final volume and then suspended at a concentration of 200 ppm inpurified water containing 250 ppm of the surfactant Trem 14 (polyhydricalcohol esters). This suspension was sprayed to the point of run-off onwheat seedlings. The following day the seedlings were inoculated with aspore suspension of Plasmopara viticola (the causal agent of grapedowney mildew) and incubated in a saturated atmosphere at 20° C. for 24hours, and then moved to a growth chamber at 20° C. for 6 days, and thenincubated in a saturated atmosphere at 20° C. for 24 hours, after whichdisease ratings were made. Of the compounds tested, the following gave70% disease control or higher when tested at 40 ppm: 1, 6, 15, 17, 18,19, 20, 22, 25, 30, 32, 35, 36, 38, 40, 41, 49, 52, 54, 55, 56, 57, 58,59, 60, 61, 62, 65, 73, 74, 75, 76, 78.

What is claimed is:
 1. A compound of the formula: ##STR41## wherein: Qis selected from the group ##STR42## A is selected from the group C₁ -C₅alkylene and C₃ -C₆ cycloalkylene, where any one atom of A can beoptionally substituted with R¹ ;X is Si or Ge; R¹ is selected from thegroup C₁ -C₂ haloalkyl, CN, C(O)R⁸, CO₂ R⁸, C(O)N(R⁸)R⁹, N₃, NO₂,N(R⁸)R⁹, N(R⁸)C(O)R⁹, N(R⁸)C(O)N(R¹⁰)R⁹, N(R⁸)S(O₂ R¹⁰, OR⁸, OC(O)R⁸,OCO₂ R⁸, OC(O)N(R⁸)R⁹, OS(O)₂ R⁸, SR⁸, S(O) R⁸, S(O)₂ R⁸ and SCN;provided that when R¹ is N(R⁸)S(O)₂ R¹⁰, then R¹⁰ is other than H andwhen R¹ is OC(O)R⁸, OCO₂ R⁸, OS(O)₂ R⁸, S(O)R⁸ or S(O)₂ R⁸, then R⁸ isother than H; R² is selected from the group H, halogen, C₁ -C₄ alkyl andC₁ -C₄ haloalkyl; R³ is selected from the group H, halogen, C₁ -C₆alkyl, C₁ -C₆ haloalkyl, C₂ -C₆ alkoxyalkyl and C₂ -C₆ alkylthioalkyl;R⁴ is selected from the group halogen, C₁ -C₆ alkyl, C1-C₆ haloalkyl, C₂-C₆ alkoxyalkyl and C₂ -C₆ alkylthioalkyl; R⁵ is selected from the groupH, HCO, C₂ -C₆ alkoxyalkyl C₂ -C₆ alkylcarbonyl , C₂ -C₆ alkoxycarbonyl,C₂ -C₆ haloalkoxycarbonyl, C(O) R¹⁵, R¹¹ OC(O)N(R¹²)S--, R¹¹ (R¹²)NS--,and SR⁸ ; or R⁵ is C₁ -C₆ alkyl optionally substituted with a groupselected from halogen, CN, NO₂, S(O)_(n) R¹¹, C(O)R¹¹, CO₂ R¹¹, C₁ -C₃haloalkoxy and phenyl optionally substituted by halogen, CN, or C₁ -C₂haloalkyl; R⁶ is selected from the group H, C₁ -C₆ alkyl, C₁ -C₆ alkoxy,C₂ -C₆ alkoxyalkyl, C₂ -C₆ alkoxyalkoxy, C₂ -C₆ alkenyl, C₂ -C₆haloalkenyl, C₂ -C₆ alkynyl, C₂ -C₆ alkenyloxy, C₂ -C₆ alkynyloxy, C₃-C₆ cycloalkyl, C₃ -C₆ cycloalkylalkyl, C₁ -C₆ alkylthio, C₁ -C₆alkylsulfinyl, C₁ -C₆ alkylsulfonyl, C₁ -C₆ haloalkylthio, C₁ -C₆haloalkylsulfinyl, C₁ -C₆ haloalkylsulfonyl, phenyl optionallysubstituted with W and phenoxy optionally substituted with W; R⁷ isselected from the group H, halogen, CN, NO₂, C₁ -C₂ alkyl, C₁ -C₂ alkoxyand CF₃ ; R⁸ and R¹⁰ are independently selected from the group H, C₁ -C₆alkyl, C₁ -C₆ haloalkyl, C₂ -C₆ alkenyl , C₂ -C₆ haloalkenyl, C₂ -C₆alkynyl, C₃ -C₆ haloalkynyl, C₂ -C₆ alkoxyalkyl, C₂ -C₆ alkylthioalkyl,C₁ -C₆ nitroalkyl, C₂ -C₆ cyanoalkyl, C₃ -C₈ alkoxycarbonylalkyl, C₃ -C₆cycloalkyl, C₃ -C₆ halocycloalkyl, phenyl optionally substituted with 1to 3 substituents independently selected from W and benzyl optionallysubstituted with 1 to 3 substituents independently selected from W; R⁹is selected from the group H and C₁ -C₄ alkyl; R⁸ and R⁹ can be takentogether when attached to the same atom as --(CH₂)₄ --, --(CH₂)₅ -- or--CH₂ CH₂ OCH₂ CH₂ --; R¹¹ and R¹² are independently selected from thegroup C₁ -C₄ alkyl; R¹³ is selected from the group C₁ -C₄ alkyl, C₁ -C₄alkoxyalkyl and phenyl optionally substituted with W; R¹⁴ is selectedfrom the group C₁ -C₆ alkyl, C₁ -C₆ alkoxy, C₁ -C₆ haloalkoxy, andphenyl or benzyl, each phenyl and benzyl optionally and independentlysubstituted with 1 to 3 W; R¹⁵ is selected from the group ##STR43## W isselected from the group halogen, CN, NO₂, C₁ -C₂ alkyl, C₁ -C₂haloalkyl, C₁ -C₂ alkoxy, C₁ -C₂ haloalkoxy, C₁ -C₂ alkylthio, C₁ -C₂haloalkylthio, C₁ -C₂ alkylsulfonyl and C₁ -C₂ haloalkylsulfonyl; and nis 0, 1 or 2;provided that: (i) when Q is Q-1 and A is C₁ -C₅ alkylene,then A is substituted with R¹ ; (ii) when Q is Q-1, A is C₁ -C₅ alkyleneand R¹ is OR⁸ or SR⁸, then R⁸ is other than C₁ -C₆ alkyl; (iii) when Qis Q-1 and A is C₁ -C₅ alkylene, then R¹ is other than C₁ -C₂ haloalkyl;and (iv) when Q is Q-1, R2 is chlorine, R³ is H, R⁴ is fluorine, R⁵ is Hand R⁶ and R⁷ are H, then A is other than C₂ alkylene substituted withCO₂ H.
 2. A compound according to claim 1 wherein:A is C₁ -C₅ alkylene;R¹ is selected from the group OR⁸, OC(O)R⁸ and SR⁸ ; R² is H; R³ is C₁-C₆ alkyl; R⁴ is halogen; R⁵ is selected from the group H and CH₃ ; R⁶is selected from the group C₁ -C₆ alkyl, C₂ -C₆ alkoxyalkyl, C₂ -C₆alkoxyalkoxy and phenoxy optionally substituted with W; R⁷ is selectedfrom the group H, halogen and C₁ -C₂ alkyl; R⁸ is selected from thegroup H and C₁ -C₄ alkyl; R¹¹, R¹² and R¹³ are independently selectedfrom C₁ -C₂ alkyl; R¹⁴ is selected form the group C₁ -C₄ alkyl, C₁ -C₄alkoxy and phenyl each optionally substituted with 1 to 3 W; and W isselected from the group halogen and C₁ -C₂ haloalkyl.
 3. A compoundaccording to claim 2 wherein Q is Q-1.
 4. A compound according to claim2 wherein Q is Q-2.
 5. A compound according to claim 2 wherein Q is Q-3.6. A compound according to claim 2 wherein Q is Q-4.
 7. A compoundaccording to claim 2 wherein Q is Q-5.
 8. A compound according to claim2 wherein Q is Q-6.
 9. A compound according to claim 2 wherein Q is Q-7.10. An insecticidal, acaricidal and fungicidal composition comprising aneffective amount of a compound according to any one of claims 1 to 9 anda carrier therefor.
 11. A method for controlling insects, acarids andfungi comprising applying to them or to their environment an effectiveamount of a compound according to any one of claims 1 to
 9. 12. Acompound according to claim 3:β-[(5-chloro-6-ethyl-4-pyrimidinyl)amino]-4-(1,1-dimethylethyl)-benzenepropanol.13. A compound according to claim 5:5-chloro-6-ethyl-N-[2-[4-(trimethylsilyl)phenyl]ethyl]-4-pyrimidinamine.14. A compound according to claim 5:5-chloro-6-ethyl-N-[1-[4-(trimethylsilyl)phenyl]ethyl]-4-pyrimidinamine.15. A compound according to claim 5:5-chloro-6-ethyl-N-methyl-N-[2-[4-trimethylsilyl)phenyl]-ethyl]-4-pyrimidinamine.16. A compound according to claim 5:5-chloro-6-ethyl-N-[2-[3-(trimethylsilyl)phenyl]-ethyl]-4-pyrimidinamine.17. A compound according to claim 6:5-chloro-6-ethyl-N-[2-(2-naphthalenyl)ethyl]-4-pyrimidinamine.
 18. Apesticidal composition comprising a compound according to any one ofclaims 1 to 17 and a carrier therefor.
 19. A method for controllingpests comprising applying to them or to their environment a pesticidallyeffective amount of a compound according to any one of claims 1 to 17.